Teng, Qing-Hu published the artcileDesign, syntheses and antitumor activities evaluation of 1,5-diaryl substituted pyrazole secnidazole ester derivatives, Computed Properties of 13599-22-9, the publication is Journal of Heterocyclic Chemistry (2021), 58(8), 1656-1664, database is CAplus.
According to the drug hybridization principle, a series of novel 1,5-diaryl substituted pyrazole secnidazole ester derivatives I (R1 = 4-I, 3-Me, 4-Cl, etc.; R2 = H, Me, Cl) have been synthesized by the combinations of various 1,5-diarylpyrazole-3-carboxylic acids II with secnidazole. The in vitro antitumor/cytotoxicities activities against tumor and normal cell lines, including NCI-H460 (lung tumor cell), MCG-803 (gastric tumor cell), Skov-3 (ovarian tumor cell), BEL-7404 (liver tumor cell) and HL-7702 (normal liver cell), have been evaluated using MTT assay. All compounds I showed promising inhibitory activities against four tumor cell lines. The IC50 of I (R1 = 4-I; R2 = H) against the BEL-7404 cell was 2.03μM, and those of I (R1 = 3-Me; R2 = H) against the NCI-H460, MCG-803 and Skov-3 were 1.34, 0.14, and 0.87μM, resp. All these values were much lower than those of the cisplatin. Furthermore, I (R1 = 3-Me, R2 = H; R1 = 4-I, R2 = H) were also verified to be considerably safe for normal human liver cell, since the lower IC50 values than cisplatin. Based on these results, the cell cycle anal., apoptosis ratio detection and mitochondrial membrane potential assay of I (R1 = 3-Me, R2 = H; R1 = 4-I, R2 = H) were further performed aiming to investigate their inhibition mechanism of BEL-7404 cells. It is revealed that they have effectively inhibited the cell growth by arresting the BEL-7404 cells at S phase and induced apoptosis through the mitochondria-mediated pathway.
Journal of Heterocyclic Chemistry published new progress about 13599-22-9. 13599-22-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid,Benzene, name is 1,5-Diphenyl-1H-pyrazole-3-carboxylic acid, and the molecular formula is C8H15ClN2, Computed Properties of 13599-22-9.
Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics