Canh Pham, Em; Truong, Tuyen Ngoc published the artcile< Design, Microwave-Assisted Synthesis, Antimicrobial and Anticancer Evaluation, and In Silico Studies of Some 2-Naphthamide Derivatives as DHFR and VEGFR-2 Inhibitors>, SDS of cas: 3959-07-7, the main research area is naphthamide preparation microwave antibacterial antifungal anticancer DHFR VEGFR inhibitor.
Naphthamide is a common structural framework with diverse pharmacol. activities. Ten novel 2-naphthamide derivatives I (R = 3-(morpholin-4-yl)propyl, (4-methylphenyl)methyl, (4-methoxyphenyl)methyl, (4-bromophenyl)methyl, (4-chlorophenyl)methyl; R1 = H, OMe; R2 = H, OMe; R3 = H, OMe; R4 = H, OMe) have been designed, synthesized, and evaluated for their in vitro antibacterial, antifungal, and anticancer activities. The title compounds were synthesized from dimethoxybenzaldehyde derivatives such as 2,4-dimethoxybenzaldehyde and 3,5-dimethoxybenzaldehyde through a four-step microwave-assisted synthesis process. The structures were confirmed by 1H NMR, 13C NMR, and MS spectra. Compound I [R = (4-chlorophenyl)methyl ; R1 = R3 = H; R2 = R4 = OMe] (II) showed good antibacterial activity against Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA with MIC values of 16, 16, 16, 8, and 16 μg/mL, resp., compared to ciprofloxacin (MIC = 8-16 μg/mL). Compounds I (R = (4-methylphenyl)methyl ; R1 = R3 = H; R2 = R4 = OMe)(III) (IC50 = 3.59-8.38 μM) and II (IC50 = 2.97-7.12 μM) exhibited good cytotoxic activity against C26, HepG2, and MCF7 cancer cell lines as compared to paclitaxel (IC50 = 2.85-5.75 μM). Moreover, compounds II and III exhibited better anticancer activity than PTX against the C26 cell line. In particular, compound II showed potent in vitro VEGFR-2 inhibitory activity with the IC50 value of 0.384 μM compared with sorafenib (IC50 = 0.069 μM). Therefore, compound II is the most potent compound for anticancer activity as indicated by in vitro cell line inhibition, in silico ADMET, mol. docking, and in vitro VEGFR-2 inhibition studies.
ACS Omega published new progress about Absorption. 3959-07-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H8BrN, SDS of cas: 3959-07-7.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary