Design, synthesis and biological evaluation of novel thiosemicarbazone-indole derivatives targeting prostate cancer cells was written by He, Zhang-Xu;Huo, Jin-Ling;Gong, Yun-Peng;An, Qi;Zhang, Xin;Qiao, Hui;Yang, Fei-Fei;Zhang, Xin-Hui;Jiao, Le-Min;Liu, Hong-Min;Ma, Li-Ying;Zhao, Wen. And the article was included in European Journal of Medicinal Chemistry in 2021.Electric Literature of C8H10ClNO3 The following contents are mentioned in the article:
To discover novel anticancer agents with potent and low toxicity, a range of new thiosemicarbazone-indole analogs I [R = H, Me, Cl, OMe; R1 = H, Me, R2 = H, Me, OH, etc.; R3 = H, Me; X = N, C] based on lead compound II were designed and synthesized previously. Most compounds displayed moderate to high anticancer activities against five tested tumor cells (PC3, EC109, DU-145, MGC803, MCF-7). Specifically, the represented compound I [R = H, R1 = Me; R2 = Me, R3 = H] (III) possessed strong antiproliferative potency and high selectivity toward PC3 cells with the IC50 value of 0.054μM, compared with normal WPMY-1 cells with the IC50 value of 19.470μM. Preliminary mechanism research indicated that compound (III) could significantly suppress prostate cancer cells (PC3, DU-145) growth and colony formation in a dose-dependent manner. Besides, derivative (III) induced G1/S cycle arrest and apoptosis, which may be related to ROS accumulation due to the activation of MAPK signaling pathway. Furthermore, mol. (III) could effectively inhibit tumor growth through a xenograft model bearing PC3 cells and had no evident toxicity in vivo. Overall, based on the biol. activity evaluation, analog (III) can be viewed as a potential lead compound for further development of novel anti-prostate cancer drug. This study involved multiple reactions and reactants, such as 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride (cas: 65-22-5Electric Literature of C8H10ClNO3).
3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride (cas: 65-22-5) belongs to alcohols. Under appropriate conditions, inorganic acids also react with alcohols to form esters. To form these esters, a wide variety of specialized reagents and conditions can be used. Grignard and organolithium reagents are powerful tools for organic synthesis, and the most common products of their reactions are alcohols.Electric Literature of C8H10ClNO3
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts