Derivatives of Dapsone (dap): Synthesis and Study on In Vitro Anticancer Activity and DNA Laddering Against Hep G2 and C6 Human Cancer Cell Lines

2017 ◽  
Vol 2 (16) ◽  
pp. 4382-4391 ◽  
Author(s):  
Vineeta Pillai ◽  
Rahul Kadu ◽  
Lipi Buch ◽  
Vinay K. Singh
BMB Reports ◽  
2005 ◽  
Vol 38 (5) ◽  
pp. 526-532 ◽  
Author(s):  
Vikram Dhuna ◽  
Jagmohan Singh Bains ◽  
Sukhdev Singh Kamboj ◽  
Jatinder Singh ◽  
Shanmugavel ◽  
...  

2018 ◽  
Vol 54 (2C) ◽  
pp. 502
Author(s):  
Le Duc Anh

Two new conjugates of murrayafoline A with zerumbone and artemisinin 3, 11 wereprepared by N-alkylation, in which, compound 3 was synthesized from two consecutive Nalkylationreactions. Their cytotoxicity was evaluated on four human cancer cell lines Hep-G2,LU, RD and Fl. The result showed that both compounds exhibited no activity against the testedcell lines.


2017 ◽  
Vol 12 (6) ◽  
pp. 1934578X1701200
Author(s):  
Dang Thi Tuyet Anh ◽  
Le Nhat Thuy Giang ◽  
Nguyen Thi Hien ◽  
Dinh Thi Cuc ◽  
Nguyen Ha Thanh ◽  
...  

Novel ester derivatives of betulin with AZT, d4T, and 3TC were synthesized and assessed for antitumor activities against the KB and HepG2 human cancer cell lines in vitro by MTT assay. Some derivatives displayed high anticancer properties, with IC50 values between 1 and 21 μM on the two cancer cell lines.


2018 ◽  
Vol 23 (2) ◽  
pp. 68
Author(s):  
Eti Nurwening Sholikhah ◽  
Jumina Jumina ◽  
Sitarina Widyarini ◽  
Ruslin Hadanu ◽  
Mustofa Mustofa

This research was conducted to evaluate the anticancer activity of new compounds of benzyl-1,10- phenanthroline derivatives and their selectivity. In vitro anticancer activity of 11 benzyl-1,10-phenanthroline derivatives were conducted on three human cancer cell lines, cervical cancer (HeLa), myeloma (NS-1), and breast cancer (MCF-7) using MTT-based cytotoxicity assay. The cytotoxicity of each compound was assessed to normal Vero cell line by the same method. The in vitro anticancer activity and cytotoxicity was expressed by the concentration inhibiting 50% of the cell growth (IC50), and the selectivity index (SI) was determined by calculating ratio of the IC50 on Vero cell line and the human cancer cell lines. The results showed that among the 11 compounds tested, the (1)-N-(4-butoxybenzyl)-1,10-phenanthrolinium bromide exhibited the best in vitro anticancer activity with an IC50 27.60 ± 2.76 µM on HeLa, 6.42 ± 5.53 µM on NS-1 and 9.44 ± 2.17 µM on MCF-7 cell lines. Its SI were 377.65 ± 39.97 on HeLa, 6158.72 ± 5306.34 on NS-1 and 1140.11 ± 261.85 on MCF-7 cell lines. This study demonstrated that (1)-N-(4-butoxybenzyl)-1,10-phenanthrolinium bromide possessed a potential in vitro anticancer activity on cancer cell lines with high selectivity


2011 ◽  
Vol 75 (2) ◽  
pp. 112-116 ◽  
Author(s):  
R. Manikandan ◽  
M. Beulaja ◽  
C. Arulvasu ◽  
S. Sellamuthu ◽  
D. Dinesh ◽  
...  

2020 ◽  
Vol 17 (5) ◽  
pp. 345-351
Author(s):  
Syndla Premalatha ◽  
G. Rambabu ◽  
Islavathu Hatti ◽  
Dittakavi Ramachandran

A new series of 3-(3,4,5-trimethoxyphenyl)-5-(2-(5-arylbenzo[b]thiophen-3-yl)oxa zol-5- yl)isoxazole derivatives were designed and synthesized. All these derivatives were evaluated for their anticancer activity against various human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), DU-145 (prostate cancer) and MDA MB-231 (breast cancer)-four human cancer cell lines by using MTT assay. Here, etoposide was used as a standard reference drug and most of the compounds were exhibited good anticancer activity with respect to cell lines. Among all compounds, five compounds 11b, 11c, 11f, 11i and 11j showed more potent activity than standard drug, in which, compound 11f was the most promising compound.


2020 ◽  
Vol 20 (10) ◽  
pp. 1241-1249
Author(s):  
Hong-Chuan Liu ◽  
Li-Ming Qiao ◽  
Wei Zheng ◽  
Zhao-Bao Xiang ◽  
Hai-Sheng Chen ◽  
...  

Background: Rabdosia japonica has been historically used in China as a popular folk medicine for the treatment of cancer, hepatitis, and gastricism. Glaucocalyxin A (GLA), an ent-kaurene diterpene isolated from Rabdosia japonica, is one of the main active ingredients showing potent inhibitory effects against several types of tumor cells. To the best of our knowledge, studies regarding the structural modification and Structure- Activity Relations (SAR) of this compound have not yet been reported. Objective: The aim of this study was to discover more potent derivatives of GLA and investigate their SAR and cytotoxicity mechanisms. Methods: Novel 7-O- and 14-O-derivatives of GLA were synthesized by condensation of acids or acyl chloride. The anti-tumor activities of these derivatives against various human cancer cell lines were evaluated in vitro by MTT assays. Apoptosis assays of compound 17 (7,14-diacylation product) were performed on A549 and HL-60 cells by flow cytometry and TUNNEL. The acute toxicity of this compound was tested on mice, at the dose of 300mg per kg body weight. Results: Seventeen novel 7-O- and 14-O-derivatives of GLA (1-17) were synthesized. These compounds showed potent cytotoxicity against the tested cancer cell lines, and almost all of them were found to be more cytotoxic than GLA and oridonin. Of the synthesized derivatives, compound 17 presented the greatest cytotoxicity, with IC50 values of 0.26μM and 1.10μM in HL-60 and CCRF-CEM cells, respectively. Furthermore, this compound induced weak apoptosis of A549 cells but showed great potential in stimulating the apoptosis of HL- 60 cells. Acute toxicity assays indicated that compound 17 is relatively safer. Conclusion: The results reported herein indicate that the synthesized GLA derivatives exhibited greater cytotoxicity against leukemia cells than against other types of tumors. In particular, 7,14-diacylation product of GLA was found to be an effective anti-tumor agent. However, the cytotoxicity mechanism of this product in A549 cells is expected to be different than that in other tumor cell lines. Further research is needed to confirm this hypothesis.


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