Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents

Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents Publisher

Rezaeia Z¹ ; Moghimi S² ; Javaheri R³ ; Asadi M¹ ; Mahdavi M⁴ ; Shabani S⁵ ; Edraki N⁶ ; Firuzi O⁶ ; Safavi M⁷ ; Aminia M¹ ; Asadipour A⁸ ; Zeinalzadeh E² ; Firoozpour L² ; Foroumadi A⁵

Show Affiliations

1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2. Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran
3. Department of Pharmaceutical Sciences, Islamic Azad University, Tehran, 19395, Iran
4. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
5. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran
6. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
7. Department of Biotechnology, Iranian Research Organization for Science and Technology, Tehran, 33535-111, Iran
8. Department of Medicinal Chemistry, Faculty of Pharmacy and Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran

Source: Letters in Drug Design and Discovery Published:2017

Abstract

Background: Due to the importance of 1,3,4-thiadiazoles and phthalimides in anticancer agents, a novel series of 1,3,4-thiadiazole-phthalimide system have been synthesized and evaluated in vitro against HT-29 and MCF-7 human cancer cell lines. Methods: The target compounds were prepared through four-step reaction and their cytotoxicities were evaluated by MTT assay. Results: The results showed that 4-nitrobenzoyl moiety containing derivatives are the most potent ones. The morphological evaluation also indicated that these compounds are apoptotic inducers. Conclusion: 4-Nitro-N-(5-((3-(1,3-dioxoisoindolin-2-yl)propyl)thio)-1,3,4-thiadiazol-2-yl)benzamide (8m) exhibits the best inhibitory effect against HT-29 and MCF-7 cell lines with IC50 values of 23.83 and 27.21 μM, respectively. © 2017 Bentham Science Publishers.

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Style	Citing Format
MLA	Rezaeia Z, et al.. "Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents." Letters in Drug Design and Discovery, vol. 14, no. 10, 2017, pp. 1138-1144.
APA	Rezaeia Z, Moghimi S, Javaheri R, Asadi M, Mahdavi M, Shabani S, Edraki N, Firuzi O, Safavi M, Aminia M, Asadipour A, Zeinalzadeh E, Firoozpour L, Foroumadi A (2017). Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents. Letters in Drug Design and Discovery, 14(10), 1138-1144.
Chicago	Rezaeia Z, Moghimi S, Javaheri R, Asadi M, Mahdavi M, Shabani S, Edraki N, et al.. "Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents." Letters in Drug Design and Discovery 14, no. 10 (2017): 1138-1144.
Harvard	Rezaeia Z et al. (2017) 'Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents', Letters in Drug Design and Discovery, 14(10), pp. 1138-1144.
Vancouver	Rezaeia Z, Moghimi S, Javaheri R, Asadi M, Mahdavi M, Shabani S, et al.. Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents. Letters in Drug Design and Discovery. 2017;14(10):1138-1144.
BibTex	@article{ author = {Rezaeia Z and Moghimi S and Javaheri R and Asadi M and Mahdavi M and Shabani S and Edraki N and Firuzi O and Safavi M and Aminia M and Asadipour A and Zeinalzadeh E and Firoozpour L and Foroumadi A}, title = {Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents}, journal = {Letters in Drug Design and Discovery}, volume = {14}, number = {10}, pages = {1138-1144}, year = {2017} }
RIS	TY - JOUR AU - Rezaeia Z AU - Moghimi S AU - Javaheri R AU - Asadi M AU - Mahdavi M AU - Shabani S AU - Edraki N AU - Firuzi O AU - Safavi M AU - Aminia M AU - Asadipour A AU - Zeinalzadeh E AU - Firoozpour L AU - Foroumadi A TI - Synthesis and Biological Evaluation of 1,3,4-Thiadiazole Linked Phthalimide Derivatives As Anticancer Agents JO - Letters in Drug Design and Discovery VL - 14 IS - 10 SP - 1138 EP - 1144 PY - 2017 ER -

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