1145668-26-3Relevant articles and documents
Design and synthesis of dithiocarbamate linked β-carboline derivatives: DNA topoisomerase II inhibition with DNA binding and apoptosis inducing ability
Kamal, Ahmed,Sathish, Manda,Nayak, V. Lakshma,Srinivasulu, Vunnam,Kavitha, Botla,Tangella, Yellaiah,Thummuri, Dinesh,Bagul, Chandrakant,Shankaraiah, Nagula,Nagesh, Narayana
, p. 5511 - 5526 (2015)
A series of new β-carboline-dithiocarbamate derivatives bearing phenyl, dithiocarbamate and H/methyl substitutions at position-1, 3 and 9, respectively, were designed and synthesized. These derivatives 8a-l and 13a-l and their starting precursors (7a-d and 12a-d) have been evaluated for their in vitro cytotoxic activity on selected human cancer cell lines. Among the derivatives tested, 7c, 12c, 8a, 8d, 8i, 8j, 8k, 8l and 13d-l exhibited considerable cytotoxicity against most of the tested cancer cell lines (IC50 50 values of 1.34 μM and 0.79 μM on DU-145 cancer cells, respectively. Further, the induction of apoptosis by these derivatives was confirmed by Annexin V-FITC and Hoechst staining assays. However, both biophysical as well as molecular docking studies suggested a combilexin-type of interaction between these derivatives and DNA, unlike simple β-carbolines. With a view to understand their mechanism of action, DNA topoisomerase II (topo II) inhibition assay was also performed. Overall, the present study emphasizes the importance of linking a dithiocarbamate moiety to the β-carboline scaffold for exhibiting profound activity.
Synthesis and biological evaluation of piperazine group-linked bivalent β-carbolines as potential antitumor agents
Sun, Rongqin,Liu, Rui,Zhou, Chi,Ren, Zhenghua,Guo, Liang,Ma, Qin,Fan, Wenxi,Qiu, Liqin,Yu, Huijuan,Shao, Guang,Cao, Rihui
, p. 2170 - 2174 (2015/12/11)
A series of novel bivalent β-carbolines with a piperazine group spacer between 3-methylene units were synthesized and evaluated as antitumor agents. The results demonstrated that compounds 7e and 7g exhibited the most potent cytotoxic activities against ten tumor cell lines. Structure-activity relationships analysis indicated that (1) the substituents in positions 1 and 9 of the β-carboline ring played a significant role in modulating the antitumor activity; (2) the introduction of alkyl groups into position-9 of the β-carboline nucleus enhanced their cytotoxic potencies and the butyl substituent was the optimal group. Investigation of the preliminary mechanism of action demonstrated that compound 7g showed obvious anti-angiogenic activity in the in vivo CAM assay, and the potency was similar to that of CA4P (200 μM).
Synthesis and in vitro cytotoxic evaluation of novel 3,4,5-trimethoxyphenyl substituted β-carboline derivatives
Wu, Qifeng,Cao, Rihui,Feng, Manxiu,Guan, Xiangdong,Ma, Chunming,Liu, Jinbing,Song, Huacan,Peng, Wenlie
experimental part, p. 533 - 540 (2009/09/08)
To elucidate further our SARs' study on the chemistry and cytotoxic activity and probe the structural requirement for the potent antitumor activity of β-carbolines, a series of novel 1,9-disubstituted and 1,3,9-trisubstituted β-carboline derivatives were
