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. 2012 Jul 25;17(8):8762-72.
doi: 10.3390/molecules17088762.

Synthesis and cytotoxicity testing of new amido-substituted triazolopyrrolo[2,1-c][1,4]benzodiazepine (PBDT) derivatives

Kumaraswamy Sorra  1 , Chi-Fen Chang, Srinivas Pusuluri, Khagga Mukkanti, Min-Chiau Laiu, Bo-Ying Bao, Chia-Hao Su, Ta-Hsien Chuang
Affiliations

Synthesis and cytotoxicity testing of new amido-substituted triazolopyrrolo[2,1-c][1,4]benzodiazepine (PBDT) derivatives

Kumaraswamy Sorra et al. Molecules. .

Abstract

A series of amido-substituted triazolopyrrolo[2,1-c][1,4]benzodiazepine (PBDT) derivatives was synthesized from isatoic anhydride, and their cytotoxicity against the MRC-5 and Mahlavu cell lines was evaluated. The results suggest that compound PBDT-7i with the meta-trifluoromethylbenzoyl substituent can selectively inhibit the growth of Mahlavu cells and has low toxicity towards MRC-5 cells.

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Figures

Figure 1
Figure 1
Members of the benzodiazepine family.
Scheme 1
Scheme 1
Synthesis of triazolo-fused PBD and derivatives.
Figure 2
Figure 2
PBDT-7a–k induced the death of Mahlavu cells. The concentration-dependent effects of PBDT-7a–k on human hepatocellular carcinoma cells. Mahlavu cells were treated with PBDT-7 series compounds for 48 h, and survival was assessed using a CCK-8 assay (mean ± SEM, n = 6).
Figure 3
Figure 3
The cytotoxicity assay of PBDT-7a–k against MRC-5 cells. The concentration-dependent effect of PBDT-7a–k on normal human fibroblast cells. MRC-5 cells were treated with PBDT-7 series compounds for 48 h, and survival was assessed using a CCK-8 assay (mean ± SEM, n = 6).
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