Brossard, Dominique’s team published research in European Journal of Medicinal Chemistry in 45 | CAS: 87179-40-6

European Journal of Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, HPLC of Formula: 87179-40-6.

Brossard, Dominique published the artcileSynthesis of bile acid derivatives and in vitro cytotoxic activity with pro-apoptotic process on multiple myeloma (KMS-11), glioblastoma multiforme (GBM), and colonic carcinoma (HCT-116) human cell lines, HPLC of Formula: 87179-40-6, the publication is European Journal of Medicinal Chemistry (2010), 45(7), 2912-2918, database is CAplus and MEDLINE.

The use of nitrogenous heterocycles as building blocks in the synthesis of conjugate bile acid derivatives was described. New piperazinyl bile acid derivatives I [R7a = OH, R7b = H, R12 = OH, R24 = 4-methyl-1-piperazinylamino, 4-(trans-cinnamyl)-1-piperazinyl; R7a = H, R7b = OH, R12 = H, R24 = 4-methyl-1-piperazinylamino, 4-(trans-cinnamyl)-1-piperazinyl; R7a = OH, R7b = H, R12 = H, R24 = 4-methyl-1-piperazinylamino, 4-(trans-cinnamyl)-1-piperazinyl] were synthesized and tested in vitro against various human cancer cells (GBM, KMS-11, HCT-116). The best pro-apoptotic activity was obtained with N-(4N-cinnamylpiperazin-1-yl)-3α,7β-dihydroxy-5β-cholan-24-amide I [R7a = H, R7b = OH, R12 = H, R24 = 4-(trans-cinnamyl)-1-piperazinyl] and N-(4N-cinnamyllpiperazin-1-yl)-3α,7α-dihydroxy-5β-cholan-24-amide I [R7a = OH, R7b = H, R12 = H, R24 = 4-(trans-cinnamyl)-1-piperazinyl] on these human cancer cell lines (IC50: 8.5-31.4 μM). This activity was associated with nuclear and DNA fragmentation, demonstrating that I [R7a = H, R7b = OH, R12 = H, R24 = 4-(trans-cinnamyl)-1-piperazinyl] induces cell death by an apoptotic process as does I [R7a = OH, R7b = H, R12 = H, R24 = 4-(trans-cinnamyl)-1-piperazinyl]. This study shows the possibility of heterocycle-steroids as new anticancer agents with improved bioactivity and easy to synthesize.

European Journal of Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, HPLC of Formula: 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics