Category: 5004-88-6

Ogita, Haruhisa; Isobe, Yoshiaki; Takaku, Haruo; Sekine, Rena; Goto, Yuso; Misawa, Satoru; Hayashi, Hideya published the artcile< Synthesis and structure-activity relationship of diarylamide urea derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells>, Computed Properties of 5004-88-6, the main research area is diarylamide urea Tranilast analog preparation vascular cell proliferation.

A series of diarylamide urea derivatives were synthesized and evaluated for their inhibitory activities against human coronary artery smooth muscle cells (SMCs) and human coronary artery endothelial cells (ECs). Compound I was superior to the lead compound, Tranilast, in terms of its potency of inhibitory activity and cell selectivity.

Bioorganic & Medicinal Chemistry published new progress about Cell proliferation. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Computed Properties of 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Li, Feng; Lu, Lei; Ma, Juan published the artcile< Acceptorless dehydrogenative condensation of o-aminobenzamides with aldehydes to quinazolinones in water catalyzed by a water-soluble iridium complex [Cp*Ir(H2O)3][OTf]2>, Computed Properties of 5004-88-6, the main research area is quinazolinone preparation green chem; aminobenzamide aldehyde acceptorless dehydrogenative condensation iridium complex catalyst.

A general and efficient method for the synthesis of quinazolinones, e.g., I via acceptorless dehydrogenative condensation of o-aminobenzamides with aldehydes in water has been accomplished. In the presence of [Cp*Ir(H2O)3][OTf]2, a variety of desirable products were obtained in high yields with high atom economy under environmentally benign conditions. Notably, this research will facilitate the progress of acceptorless dehydrogenative reactions in water catalyzed by water-soluble organometallic complexes.

Organic Chemistry Frontiers published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Computed Properties of 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Li, Feng; Lu, Lei; Liu, Pengcheng published the artcile< Acceptorless Dehydrogenative Coupling of o-Aminobenzamides with the Activation of Methanol as a C1 Source for the Construction of Quinazolinones>, HPLC of Formula: 5004-88-6, the main research area is dehydrogenative coupling aminobenzamide methanol iridium catalyst; quinazolinone preparation dehydrogenative coupling aminobenzamide methanol iridium catalyst.

A strategy for the synthesis of quinazolinones I (R = H, 7-Me, 6-MeO, 8-F, etc.) via acceptorless coupling of o-aminobenzamides with methanol has been accomplished in the presence of the metal-ligand bifunctional catalyst [Cp*Ir(2,2′-bpyO)(H2O)]. Notably, this research exhibited the potential of transition-metal-catalyzed activation of methanol as a C1 source for the construction of heterocycles.

Organic Letters published new progress about Benzamides Role: RCT (Reactant), RACT (Reactant or Reagent) (o-aminobenzamides). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, HPLC of Formula: 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Raffa, Demetrio; Maggio, Benedetta; Raimondi, Maria Valeria; Cusimano, Maria Grazia; Amico, Giandomenico; Carollo, Anna; Conaldi, Pier Giulio; Bai, Ruoli; Hamel, Ernest; Daidone, Giuseppe published the artcile< 2-Cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido)benzamides: synthesis, antiproliferative activity, and mechanism of action>, Formula: C9H12N2O3, the main research area is cinnamamido phenylpropiolamido phenylpropanamidobenzamide preparation anticancer; 2-(3-Phenylpropanamido)benzamides; 2-(3-Phenylpropiolamido)benzamides; 2-Cinnamamidobenzamides; Antiproliferative activity; Apoptosis; DYCGFIFOMKVDQP-UHFFFAOYSA-N; GAEWJVNXMYWFOT-FPYGCLRLSA-N; GLOIPBXNPXFMCD-CMDGGOBGSA-N; GTMVKWANDDSBPP-UHFFFAOYSA-N; GUWKFLZAMNTMFA-UHFFFAOYSA-N; IBBGALVVPWZGNP-JXMROGBWSA-N; IRYCZCAWVJZWKT-QPJJXVBHSA-N; JZURWIGFELHAQF-UHFFFAOYSA-N; LIWFXFAWCAUFBU-UHFFFAOYSA-N; LRIOFNWWMBLPSV-RMKNXTFCSA-N; MTEXNJMFEMIDJZ-CSKARUKUSA-N; MVXMFTXNNUIRAF-UHFFFAOYSA-N; MWHVYZNXRYFKFD-UHFFFAOYSA-N; OEHLQIRCXNADOK-JXMROGBWSA-N; PIQFLKOEQNXADK-QPJJXVBHSA-N; QUNOMTLXTSUWOB-CMDGGOBGSA-N; RHBJSXACCJTPRE-UHFFFAOYSA-N; USJUKEPNAZAKSG-UHFFFAOYSA-N; WMHHXKMPUMTPIJ-RMKNXTFCSA-N; WPPDXKZWCFUROB-UHFFFAOYSA-N; XMXNTDIXMAUMEJ-UHFFFAOYSA-N; ZLNSPXKNAWBJIG-ZHACJKMWSA-N; ZXBUZBGNIFHLGX-UHFFFAOYSA-N.

Several new benzamides were synthesized by stirring in pyridine the acid chlorides with the appropriate anthranilamide derivatives Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human chronic myelogenous leukemia cells, MCF-7 breast cancer cells, HTC-116 and HT26 colon cancer cells and NCI H460 non-small cell lung cancer cells).

European Journal of Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Formula: C9H12N2O3.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Ogawa, Nobuo; Yoshida, Toshihiko; Aratani, Takayuki; Koshinaka, Eiichi; Kato, Hideo; Ito, Yasuo published the artcile< Synthesis and histamine H2-antagonist activity of 4-quinazolinone derivatives>, Quality Control of 5004-88-6, the main research area is piperidinylmethylphenoxypropylaminoquinazolinone preparation antiulcer histamine antagonist; quinazolinone piperidinylmethylphenoxypropylamino preparation histamine antagonist; structure activity aminomethylphenoxyalkylaminoquinazolinone histamine antagonist.

With the aim of developing new antiulcer agents, a series of 4-quinazolinone derivatives e.g., I (R = piperidino, pyrrolidino, morpholino, R1 = H, OMe, R2 = H, Me; n = 2, 3, 4) was synthesized and tested for histamine H2-antagonist activity and gastric antisecretory activity. Thus, 2-alkylamino-, 2-alkylthio-, and 2-alkyl-4-quinazolinones were prepared by the condensation of alkylamines with 2-chloro- or 2-methylthio-4-quinazolinones, the condensation of alkyl bromides with 2-mercapto-4-quinazolinones, and the condensation of alkylcarboxylic acids with anthranilamides, resp. Several of the 4-quinazolinone derivatives showed potent H2-antagonist activity, and one of them, I (R = piperidino, R1 = R2 = H, n = 3), showed the most potent antisecretory activity. The structure-activity relationships are discussed.

Chemical & Pharmaceutical Bulletin published new progress about Histamine H2 receptor antagonists. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Quality Control of 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Wang, Chao-Jie; Guo, Xinxin; Zhai, Rui-Qin; Sun, Changning; Xiao, Guokai; Chen, Jin; Wei, Mei-Yan; Shao, Chang-Lun; Gu, Yuchao published the artcile< Discovery of penipanoid C-inspired 2-(3,4,5-trimethoxybenzoyl)quinazolin-4(3H)-one derivatives as potential anticancer agents by inhibiting cell proliferation and inducing apoptosis in hepatocellular carcinoma cells>, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide, the main research area is trimethoxybenzoyl quinazolinone anticancer discovery preparation human apoptosis; Apoptosis; Cell cycle; Hepatocellular carcinoma; Penipanoid C; Quinazoline.

Hepatocellular carcinoma (HCC) is the most common form of liver cancer and the fourth leading cause of cancer-related death worldwide. First-line drugs such as sorafenib provide only a modest benefit to HCC patients. In this study, the gram-scale synthesis of 2-benzoylquinazolin-4(3H)-one skeleton was achieved successfully via the I2/DMSO catalytic system. A series of penipanoid C-inspired 2-(3,4,5-trimethoxybenzoyl)quinazolin-4(3H)-one derivatives was synthesized and evaluated for their cytotoxic activities against four cancer cell lines, HepG2, Bel-7402, A549, and U251. Among these compounds, I was the most effective one with IC50 values of 1.22μM and 1.71μM against HepG2 and Bel-7402 cells, resp. Mechanistic studies showed that I inhibited hepatocellular carcinoma cell proliferation via arresting cell cycle. Addnl., I induced HepG2 cells apoptosis by inducing reactive oxygen species production and elevating the expression of apoptosis-related proteins. More importantly, I displayed significant in vivo anticancer effects in the HepG2 xenograft models. This suggests that I is a promising lead compound with the potential to be developed as a chemotherapy agent for hepatocellular carcinoma.

European Journal of Medicinal Chemistry published new progress about Acetophenones Role: RCT (Reactant), RACT (Reactant or Reagent). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Asano, Toru; Yoshikawa, Tomohiro; Nakamura, Hiroyuki; Uehara, Yoshimasa; Yamamoto, Yoshinori published the artcile< Synthesis and biological evaluation of benzamides and benzamidines: structural requirement of a pyrimidine ring for inhibition of EGFR tyrosine kinase>, HPLC of Formula: 5004-88-6, the main research area is benzamide benzamidine preparation epidermal growth factor receptor tyrosine kinase.

The benzamides I (R = cyclohexyl, 3-BrC6H4, 2-pyridyl, etc.) benzamidines II (R1 = 3-BrC6H4, 3-ClC6H4, 3-MeOC6H4, 3-chloro-4-fluorophenyl), and protected benzamidines (III, same R1) were synthesized as the mimics of 4-anilinoquinazolines, which possess inhibition of epidermal growth factor receptor (EGFR) tyrosine kinase, and were tested for cytotoxicity toward A431 and inhibitory activity toward autophosphorylation by the enzyme assay. High cell growth inhibition was observed in a series of the cyclic benzamides III: the IC50 values are 0.09-0.32 mM. The benzamidines III (R1 = 3-BrC6H4, 3-ClC6H4) exhibited high inhibition of EGFR tyrosine kinase at a 1.0 μM concentration, although the benzamides I and the benzamidines II did not show significant kinase inhibition at a 10 μM concentration

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, HPLC of Formula: 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Venkateswarlu, Somepalli; Satyanarayana, Meka; Murthy, Gandrothu Narasimha; Siddaiah, Vidavalur published the artcile< Cyclisation of 2-(2-aminophenyl)quinazolin-4(3H)-one reexamined: formation of isomeric angular fused quinazolinoquinazolinones and their spectroscopic identification>, Reference of 5004-88-6, the main research area is aminophenylquinazolinone acetic anhydride cyclization; isomeric angular fused quinazolinoquinazolinone preparation IR NMR.

Cyclization of 2-(2-aminophenyl)quinazolin-4(3H)-ones on N3 and on N1 leading to 6-alkyl-(8H)-quinazolino[4,3-b]quinazolin-8-ones and 6-alkyl-(13H)-quinazolino[3,4-a]quinazolin-13-ones, resp. was described for the first time. The differences in the IR and carbon NMR data of these isomeric fused quinazolinoquinazolinones afford a useful method for distinguishing between the two series.

Tetrahedron Letters published new progress about Anhydrides Role: RCT (Reactant), RACT (Reactant or Reagent). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Reference of 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Yadav, Mange R.; Grande, Fedora; Chouhan, Bishram S.; Naik, Prashant P.; Giridhar, Rajani; Garofalo, Antonio; Neamati, Nouri published the artcile< Cytotoxic potential of novel 6,7-dimethoxyquinazolines>, Related Products of 5004-88-6, the main research area is dimethoxyquinazoline preparation; cancer anticancer cytotoxicity human structure activity.

The synthesis and cytotoxicity of a series of substituted 6,7-dimethoxyquinazoline derivatives, e.g., I, is reported. The cytotoxic activity of all synthesized compounds has been evaluated against HCT116p53+/+ and HCT116p53-/- colon cancer cells and a HEY ovarian cancer cell line naturally resistant to cisplatin. Nine of the tested compounds showed significant cytotoxicity in all cell lines at 10 μM. The most promising derivative I showed IC50values of 0.7 and 1.7 μM in the two colon cancer cell lines.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Related Products of 5004-88-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Althuis, T. H.; Moore, P. F.; Hess, H. J. published the artcile< Development of ethyl 3,4-dihydro-4-oxopyrimido[4,5-b]quinoline-2-carboxylate, a new prototype with oral antiallergy activity>, Formula: C9H12N2O3, the main research area is quinazolinecarboxylate analog preparation antiallergic; allergy inhibitor quinazolinecarboxylate analog; cromoglycate analog allergy inhibitor.

The synthesis and antiallergic activity is described of 18 3,4-dihydro-4-oxoquinazoline-2-carboxylic acid analogs I (R = H, MeO, NO2, Br, etc.; R1 = H or Et; X = CH or N) and II (R = H, CO2Na, CO2Et, OH, etc.; X = CH or N). The title compound II (R = CO2Et, X = N) [55149-04-7] was 10 times more potent (ED50 = 3 mg/kg, orally) than di-Na cromoglycate in the rat passive cutaneous anaphylaxis test. Structure-activity relations are discussed.

Journal of Medicinal Chemistry published new progress about Allergy. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Formula: C9H12N2O3.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics