An article 2-Styryl-4-aminoquinazoline derivatives as potent DNA-cleavage, p53-activation and in vivo effective anticancer agents WOS:000509616800015 published article about MUTANT P53; CANCER-CELLS; CP-31398; RESEARCHES; GROWTH; IDENTIFICATION; INHIBITORS; BINDING; PROTEIN; TARGET in [Wei, Xin-Wei; Yuan, Jing-Mei; Chen, Nan-Ying; Li, Xiao-Juan; Pan, Cheng-Xue; Mo, Dong-Liang; Su, Gui-Fa] Guangxi Normal Univ, Sch Chem & Pharmaceut Sci, State Key Lab Chem & Mol Engn Med Resources, Guilin 541004, Peoples R China; [Huang, Wan-Yun] Guilin Med Univ, Dept Pharmacol, Guilin 541004, Peoples R China in 2020, Cited 39. Safety of 2-Aminobenzamide. The Name is 2-Aminobenzamide. Through research, I have a further understanding and discovery of 88-68-6
Forty-eight analogues of CP-31398, an antitumor agent modulated the mutant p53 gene were synthesized and their cytotoxicities against four cancer cell lines with different p-53 status including bladder cell 724 (w-p53), gastric cell MGC-803 (m-p53), prostate cell DU145 (m-p53), prostate cell PC-3 (null-p53), lung cell A549 (w-p53) and normal liver cell line HL-7702 (w-p53) were examined. (E)-2-(4-Nitrostyryl)-4-(3-dimethylaminopropyl)-aminoquinazoline (10ah) was identified as the most potent compound in anti-proliferation against MGC-803 cells, with IC50 lowed to 1.73 mu M, far potency than that of CP-31398. Molecular mechanism study revealed that 10ah and CP-31398 differ greatly in mechanism to exert their antitumor properties. 10ah could intercalate into DNA and resulted in significant DNA double-strand break 10ah-treatment in MGC-803 cells increased the expression of p53, phosphorylated p53 (p-p53), CDK4, p21 to cause cell cycle arrest at G2/M phase, significantly up-regulated the levels of pro-apoptosis proteins Bak, Bax, Bim while down-regulated the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1, fluctuated the intracellular reactive oxygen species (ROS), Ca2+ and mitochondria! membrane potential, activated Caspase-9 and Caspase-3 to induce apoptosis. 10ah also displayed potent anticancer efficiency against MGC-803 xenograft tumors models, with tumor growth inhibition (TGI) up to 61.8% at 20 mg/kg without obvious toxicity. (C) 2019 Elsevier Masson SAS. All rights reserved.
Welcome to talk about 88-68-6, If you have any questions, you can contact Wei, XW; Yuan, JM; Huang, WY; Chen, NY; Li, XJ; Pan, CX; Mo, DL; Su, GF or send Email.. Safety of 2-Aminobenzamide
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Thiomorpholine – Wikipedia,
,Thiomorpholine | C4H9NS – PubChem