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NP lee wa s eJ od uo r nn oa tl aod fj uC s ht em ma ri sg it nr ys
DOI: 10.1039/C7NJ00338B
Journal Name
ARTICLE
Synergy studies
Alves, S. Thurow, R. Webber, G. Perin, E. J. Lenardão, Tet.
Lett. 2013, 54, 3215-3218.
The synergistic effect of compound 5e with well-known
antibacterial drugs (KAN, RIF) and antifungal drug (Amp B) were 8. D. Plano, D. N. Karelia, M. K. Pandey, J. E. Spallholz, S. Amin,
evaluated using the checkerboard test performed in triplicate A. K. Sharma, J. Med. Chem. 2016, 59, 1946-1959.
and the results were expressed in terms of fractional inhibitory 9. Y. Y. Zhang, R. F. Zhang, S. L. Zhang, S. Cheng, Q. L. Li, C. L.
concentration (FIC) which is ratio of the MIC of drug in Ma, Dalton Trans., 2016, 45, 8412-8421.
combination to the MIC of drug alone. The fractional inhibitory 10. S. Kumar, J. Yan, J. Poon, V. P. Singh, X. Lu, M. K. Ott, L.
concentration index is sum of FIC’s of different interacting
species (FICI = ΣFIC = FIC + FIC ) and it describes extent of
Engman, S. Kumar, Angew. Chem. Int. Ed. 2016, 55, 3729-
A
B
3733.
interaction between two drugs. The interaction considered to be 11. B. M. Gai, A. L. Stein, J. A. Roehrs, F. N. Bilheri, C. W.
synergistic if value of FICI ≤ 0.5, and as antagonistic when > 4.0,
and any value in between as indifferent.
Nogueira, G. Zeni, Org. Biomol. Chem., 2012, 10, 798-807.
12. Y. Kotaiah, N. Harikrishna, K. Nagaraju, D. V. R. Sai Gopal, V.
Taranath, C. V. Rao, J. Chem. Pharm. Res., 2013, 5, 359-369.
Cytotoxicity analysis
13. M. Ninomiya, D. R. Garud, M. Koketsu, Coord. Chem. Rev.
2011, 255, 2968-2990.
Cytotoxicity analysis of compounds 5d, 5e, 5g and 5k against HEK-
2
93 (normal human embryonic kidney cells) and HeLa (cervical 14. B. J. Bhuyan, G. Mugesh, Org. Biomol. Chem., 2011,
cancer cells) was performed using MTT (3-(4,5)-dimethylthiazol-2- 5192.
yl)-2,5-diphenyl tetrazolium bromide) protocol. In typical 15. a) N. Sharma, S. Kumar, I. K. Maurya, K. K. Bhasin, A. Verma,
N. Wangoo, A. K. K. Bhasin, S. K. Mehta, S. Kumar, R. K.
Sharma, RSC Adv. 2016, , 114224–114234; b) R. A. Hussain,
9, 5185-
a
4
procedure, the cells (5x10 /well) were cultured in RPMI-1640
medium supplemented with 10% fetal bovine serum in the 96-well
6
0
microtiter plate at 37 C overnight. Then all the compounds at their
A. Badshah, J. M. Pezzuto, N. Ahmed, T. P. Kondratyuk, E.
Park, J. Photochem. Photobiol. B: 2015, 148, 197–208; c) Z.
Wen, J. Xu, Z. Wang, H. Qi, Q. Xu, Z. Bai, Q. Zhang, K. Bao, Y.
Wu, W. Zhang, Eur. J. Med. Chem. 2015, 90, 184‒194
0
MIC were added to the cells in separate wells and incubated at 37 C
0
for 18 hours followed by further incubation at 37 C for 3 to 5h in
20µl of MTT solution (5 mg/ml) in PBS. The supernatant (120µl) was
removed, 100µl DMSO was added and the resulting suspension was 16. J. P. Paolini, R. K. Robins, J. Org. Chem. 1965, 30, 4085-4090
mixed to dissolve the formazan crystals. The percent viability of 17. a) X. Zhou, H. Yan, C. Ma, Y. He, Y. Li, J. Cao, R. Yan, G. Huang,
cells was calculated by the ratio of O.D570 of treated cells to the
O.D570 of untreated cells. Untreated cells and 10% dimethyl
sulfoxide (DMSO) were taken as negative and positive control
respectively.
J. Org. Chem. 2016, 81, 25-31; b) H. Cao, H. Zhan, Y. Lin, X.
Lin, Z. Du, H. Jiang, Org. Lett., 2012, 14, , 1688-1691; c) S. Lei,
G. Chen, Y. Mai, L. Chen, H. Cai, J. Tan, H. Cao, Adv. Synth.
Catal. 2016, 358, 67– 73; d) C. Wang, S. Lei, H. Cao, S. Qiu, J.
Liu, H. Deng, C. Yan, J. Org. Chem. 2015, 80, 12725-12732; e)
Acknowledgements
KKB is grateful to Council of Scientific & Industrial Research
S. Lei, Y. Mai, C. Yan, J. Mao, H. Cao, Org. Lett. 2016, 18,
3582-3585;
(
CSIR), India for Emeritus Scientist Scheme India 18. A. K. Bagdi, S. Santra, K. Monir, A. Hajra, Chem. Commun.,
2
2
1(0967)/13/EMR-II and UGC for research Project F. No. 43-
2015, 51, 1555-1575.
54/2014(SR). RKS thank Science & Engineering Research Board, 19. G. Li, K. Hee Jung, H. Lee, M. K. Son, J. H. Seo, S. Hong, Y.
India (SB/SO/BB/0040/2013). SK and NS also thank CSIR, India
for their senior research fellowships (grant no.
9/135/(0674)/2012/ EMR-I and 09/135(0675)/2012-EMR-I).
Jeong, S. Hong, S. Hong, Cancer Lett. 2013, 329, 59-67; b) S.
Yun, K. H. Jung, H. Lee, M. K. Son, J. Seo, H. H. Yan, B. H. Park,
S. Hong, S. Hong, Cancer Lett. 2013, 331, 250-261.
0
2
0. S. Kumar, N. Sharma, I. K. Maurya, A. K. K. Bhasin, N.
Wangoo, P. Brandão, V. Félix, K. K. Bhasin, R. K. Sharma, Eur.
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