In 2022,Zhidkov, Maxim E.; Kaune, Moritz; Kantemirov, Alexey V.; Smirnova, Polina A.; Spirin, Pavel V.; Sidorova, Maria A.; Stadnik, Sergey A.; Shyrokova, Elena Y.; Kaluzhny, Dmitry N.; Tryapkin, Oleg A.; Busenbender, Tobias; Hauschild, Jessica; Rohlfing, Tina; Prassolov, Vladimir S.; Bokemeyer, Carsten; Graefen, Markus; von Amsberg, Gunhild; Dyshlovoy, Sergey A. published an article in Marine Drugs. The title of the article was 《Study of Structure-Activity Relationships of the Marine Alkaloid Fascaplysin and Its Derivatives as Potent Anticancer Agents》.Category: esters-buliding-blocks The author mentioned the following in the article:
Marine alkaloid fascaplysin and its derivatives are known to exhibit promising anticancer properties in vitro and in vivo. However, toxicity of these mols. to non-cancer cells was identified as a main limitation for their clin. use. Here, for the very first time, we synthesized a library of fascaplysin derivatives covering all possible substituent introduction sites, i.e., cycles A, C and E of the 12H-pyrido[1-2-a:3,4-b′]diindole system. Their selectivity towards human prostate cancer vs. non-cancer cells, as well as the effects on cellular metabolism, membrane integrity, cell cycle progression, apoptosis induction and their ability to intercalate into DNA were investigated. A pronounced selectivity for cancer cells was observed for the family of di- and trisubstituted halogen derivatives (modification of cycles A and E), while a modification of cycle C resulted in a stronger activity in therapy-resistant PC-3 cells. Among others, 3,10-dibromofascaplysin exhibited the highest selectivity, presumably due to the cytostatic effects executed via the targeting of cellular metabolism Moreover, an introduction of radical substituents at C-9, C-10 or C-10 plus C-3 resulted in a notable reduction in DNA intercalating activity and improved selectivity. Taken together, our research contributes to understanding the structure-activity relationships of fascaplysin alkaloids and defines further directions of the structural optimization. After reading the article, we found that the author used Diethyl 2-methylmalonate(cas: 609-08-5Category: esters-buliding-blocks)
Diethyl 2-methylmalonate(cas: 609-08-5) belongs to aliphatic hydrocarbons. Aliphatic hydrocarbons belong to the most abundant fraction in crude oil. Aliphatics molecules are linear or branched open-chain structures such as n-alkanes, isoalkanes, cycloalkanes (naphthenes), terpenes and steranes.Category: esters-buliding-blocks
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics