Name: 2,5-Dimethoxybenzaldehyde. In 2019.0 BIOORG CHEM published article about PNEUMOCYSTIS-CARINII; METHOTREXATE; POTENT; DERIVATIVES; PIRITREXIM; SERIES; AGENTS in [Abdelaziz, Ola A.; El Husseiny, Walaa M.; Selim, Khalid B.; Eisa, Hassan M.] Mansoura Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Mansoura 35516, Egypt in 2019.0, Cited 46.0. The Name is 2,5-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 93-02-7.
A new series of pyrido[2,3-d] pyrimidines 3-18 bearing substitution at C-5 position was synthesized. All compounds were tested for their in vitro antitumor activity against five human cancer cell lines namely; hepatocellular carcinoma (HePG2), breast carcinoma (MCF-7), human prostate carcinoma (PC3), colorectal carcinoma (HCT-116), and cervical carcinoma (Hela) using doxorubicin as a positive control. Compounds 3, 4, 9, 11, 13, 14, 15 and 17 exhibited the highest antitumor activity against the tested cell lines and were selected to screen their enzymatic inhibition against dihydrofolate reductase enzyme (DHFR) compared with the reference drug methotrexate (MTX), to explain the probable mechanism of action of the observed anticancer activity. Compound 11 displayed the highest inhibitory activity (IC50 = 6.5 mu M) among the tested compounds in comparison with MTX (IC50 = 5.57 mu M). Also, compounds 13 and 14 showed high inhibitory activity against DHFR with IC50 values 7.1 and 8.7 mu M, respectively. Comparative molecular modeling study was performed between DHFR inhibitors 11, 13 and 14 of the highest activity and 10 of the lowest activity among the eight inhibitors against MTX. Docking studies into the active site of DHFR domain showed good agreement with the obtained biological results. Finally, compound 11 was found to be best antitumor, DHFR inhibitor, and it induced the process of apoptosis at Pre-G phase and cell cycle arrest at G2/M phase in MCF-7 cells.
About 2,5-Dimethoxybenzaldehyde, If you have any questions, you can contact Abdelaziz, OA; El Husseiny, WM; Selim, KB; Eisa, HM or concate me.. Name: 2,5-Dimethoxybenzaldehyde
Reference:
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