Category: 5004-88-6

Lai, Kuo-Chu; Chia, Yi-Ting; Yih, Ling-Huei; Lu, Yi-Liang; Chang, Shih-Ting; Hong, Zi-Xuan; Chen, Tai-Lin; Hour, Mann-Jen published the artcile< Antitumor effects of the novel quinazolinone Holu-12: induction of mitotic arrest and apoptosis in human oral squamous cell carcinoma CAL27 cells>, Name: 2-Amino-4,5-dimethoxybenzamide, the main research area is quinazolinone mitotic arrest human oral squamous cell carcinoma apoptosis; 5-FU sensitivity; Quinazolinone derivatives; apoptosis; human oral squamous cell carcinoma; mitotic arrest.

Quinazolinone is a privileged chem. structure employed for targeting various types of cancer. This study aimed to demonstrate the antitumor activity of synthesized 6,7-disubstituted-2-(3-fluorophenyl) quinazolines (HoLu-11 to HoLu-14). The cytotoxicity was assessed by the sulforhodamine B (SRB) assay. The cell cycle was examined by flow cytometry. The expression levels of cell cycle- and apoptosis-related proteins were estimated by western blotting. A xenograft animal model was used to explore the antitumor effects of HoLu-12. Among four synthetic quinazolinone derivatives, HoLu-12 significantly reduced the viability of oral squamous cell carcinoma (OSCC) cells. HoLu-12 induced G2/M arrest and increased the expression of cyclin B, histone H3 (Ser10) phosphorylation, and cleaved PARP, indicating that HoLu-12 could induce mitotic arrest and then apoptosis. Moreover, the combination of HoLu-12 and 5-fluorouracil (5-FU) displayed synergistic toxic effect on OSCC cells. HoLu-12 significantly inhibited tumor growth in vivo. HoLu-12 induces mitotic arrest and leads to apoptosis of OSCC cells. Furthermore, HoLu-12 alone or in combination with 5-FU is a potential therapeutic agent for OSCC.

Anticancer Research published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Name: 2-Amino-4,5-dimethoxybenzamide.

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

Patil, Nitin T.; Kavthe, Rahul D.; Raut, Vivek S.; Shinde, Valmik S.; Sridhar, Balasubramanian published the artcile< Gold- and Platinum-Catalyzed Formal Markownikoff's Double Hydroamination of Alkynes: A Rapid Access to Tetrahydroquinazolinones and Angularly-Fused Analogues Thereof>, Application of C9H12N2O3, the main research area is alkynol aminobenzamide gold platinum Markownikoff hydroamination; tetrahydroquinazolinone preparation; angularly fused hexahydropyrroloquinazolinone preparation; Markownikoff hydroamination catalyst gold platinum.

A highly efficient gold(I)- and platinum(II)-catalyzed process for formal Markownikoff’s double hydroamination of alkynes tethered with hydroxyl group has been developed. The method was shown to be applicable to a broad range of 2-aminobenzamides and alkynols leading to the formation of multiply substituted tetrahydroquinazolinones. Interestingly, when Pt(IV)Cl4 catalyst was employed, cyclic angularly fused compound was obtained.

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

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

Zhu, Yan-ping; Fei, Zhuan; Liu, Mei-cai; Jia, Feng-cheng; Wu, An-xin published the artcile< Direct One-Pot Synthesis of Luotonin F and Analogues via Rational Logical Design>, Application of C9H12N2O3, the main research area is luotonin F synthesis iodination Kornblum oxidation annulation; quinazolinone acyl derivative preparation.

An efficient one-pot synthetic protocol has been proposed for the synthesis of luotonin F [2-(3-quinolinylcarbonyl)-4(1H)-quinazolinone] from easily available starting materials. Through a rational logical design, multifundamental reactions (iodination, Kornblum oxidation, and annulation) were assembled in one-pot. The developed approach can efficiently synthesize luotonin F and a diversity of analogs.

Organic Letters published new progress about Cyclization. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Application of C9H12N2O3.

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

Lee, Seohoo; Sim, Jaeuk; Jo, Hyeju; Viji, Mayavan; Srinu, Lanka; Lee, Kiho; Lee, Heesoon; Manjunatha, Vishwanath; Jung, Jae-Kyung published the artcile< Transition metal-free synthesis of quinazolinones using dimethyl sulfoxide as a synthon>, HPLC of Formula: 5004-88-6, the main research area is quinazolinone preparation transition metal free microwave irradiation; dimethyl sulfoxide aminobenzamide intramol oxidative annulation.

Biol. important quinazolinones have been synthesized from 2-aminobenzamides and DMSO. The key feature of the reaction is the utilization of DMSO as a methine source for intramol. oxidative annulation. The CNS depressant drug methaqualone has also been synthesized by this methodol. The present method involves the synthesis of quinazolinones with a broad substrate scope and a good yield.

Organic & Biomolecular Chemistry published new progress about Benzamides Role: RCT (Reactant), RACT (Reactant or Reagent) (amino). 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

Hou, Yunlei; Wu, Shasha; Ma, Longsheng; Bai, Jinying; Liu, Zijian; Zhao, Yanfang published the artcile< Design, synthesis and antitumor activity of novel 6,7-dimethoxyquinazoline derivatives containing diaryl urea moiety>, Product Details of C9H12N2O3, the main research area is sorafenib dimethoxyquinazoline diaryl urea scaffold antitumor lung gastric cancer.

A series of 6,7-dimethoxyquinazoline derivatives connected by diaryl urea scaffolds was designed, synthesized and their in vitro antitumor activities were evaluated. Most of them showed an excellent potency against the four tested cancer cell lines as compared with sorafenib. Particularly, a promising compound 20 was identified, which showed the most potent antitumor activities with IC50 values of 0.08, 0.09, 0.16 and 0.19 μmol/L against H460, HT-29, MKN-45 and MDA-MB-231 cell lines, resp. The structure-activity relationship(SAR) anal. indicated that compounds with dimethylamino or diethylamino group at the C4 position of 6,7-dimethoxyquinazoline moiety exhibited superior activities than compounds bearing morpholino groups.

Chemical Research in Chinese Universities published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Product Details of C9H12N2O3.

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

Chen, Hui; Li, Peng; Qin, Rongfei; Yan, Hong; Li, Gang; Huang, Haihong published the artcile< DMAP-Catalyzed One-Pot Synthesis of Quinazoline-2,4-diones from 2-Aminobenzamides and Di-tert-butyl Dicarbonate>, Category: amides-buliding-blocks, the main research area is quinazolinedione preparation; aminobenzamide di tert butyl dicarbonate heterocyclization DMAP catalyst.

The one-pot synthesis of quinazoline-2,4-diones was developed in the presence of 4-dimethylaminopyridine (DMAP) by metal-free catalysis. The com. available (Boc)2O acted as a key precursor in the construction of the 2-position carbonyl of quinazolinediones. The p-methoxybenzyl (PMB)-activated heterocyclization could smoothly proceed at room temperature instead of the microwave condition. This strategy is compatible with a variety of substrates with different functional groups. Furthermore, this protocol was utilized to smoothly prepare Zenarestat with a total yield of 70%.

ACS Omega published new progress about Benzamides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (amino). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Category: amides-buliding-blocks.

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

Raffa, Demetrio; Maggio, Benedetta; Plescia, Fabiana; Cascioferro, Stella; Raimondi, Maria Valeria; Cancemi, Gabriella; D’Anneo, Antonella; Lauricella, Marianna; Cusimano, Maria Grazia; Bai, Ruoli; Hamel, Ernest; Daidone, Giuseppe published the artcile< Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality>, Formula: C9H12N2O3, the main research area is preparation acetamido benzamide derivative cancer; 2-(2-Phenoxyacetamido)benzamides; Antiproliferative activity; Apoptosis; G0/G1 arrest; Pro-caspase 3.

Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R1-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clin. isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptosis, which was mediated by caspase activation.

Bioorganic & Medicinal Chemistry published new progress about Antiproliferative agents. 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

Ogita, H.; Isobe, Y.; Takaku, H.; Sekine, R.; Goto, Y.; Misawa, S.; Hayashi, H. published the artcile< Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells>, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide, the main research area is diarylamide derivative antiproliferative SAR preparation coronary artery.

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

Bioorganic & Medicinal Chemistry Letters published new progress about Arterial endothelium, coronary artery endothelium. 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

Diaper, C. M. published the artcile< Other tetrahetero-substituted methanes>, COA of Formula: C9H12N2O3, the main research area is review hetero methane derivative preparation organic synthesis.

A review of the preparation and synthetic applications of tetrahetero-substituted methanes.

Science of Synthesis published new progress about 5004-88-6. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, COA of Formula: C9H12N2O3.

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

Venkateswarlu, Somepalli; Satyanarayana, Meka; Lakshmikanthan, Vijaybaskar; Siddaiah, Vidavalur published the artcile< Fused Quinazolinoquinazolinones: Synthesis, Isomerization, Spectroscopic Identification, and Anticancer Activity>, Quality Control of 5004-88-6, the main research area is EGFR tyrosine kinase anticancer fused quinazolino quinazolinone; fused quinazolino quinazolinone preparation anticancer.

13H-quinazolino[3,4-a]quinazolin-13-ones have been synthesized from 2-aminobenzamides in four steps. An acid-catalyzed or base-catalyzed isomerization of 13H-quinazolino[3,4-a]quinazolin-13-ones to 8H-quinazolino[4,3-b]quinazolin-8-ones in excellent yields (90-95%) has been reported. The differences in the IR and NMR (1H & 13C) data of these isomeric fused quinazolinoquinazolinones afford a useful method for distinguishing between the two series. These analogs showed moderate anticancer activity (EGFR-TK inhibition).

Journal of Heterocyclic Chemistry published new progress about Epidermal growth factor receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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