Design and Synthesis of 1,3,4-Thiadiazole Derivatives as Novel Anticancer and Antitubercular Agents

Sekhar, D. Chandra; Rao, Deepali; Rao, A. Tejeswara; Kumar, Udit; Jha, Anjali

doi:10.1134/s1070363219040224

Cited by 15 publications

(4 citation statements)

References 25 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Among them, N-benzyl-5-(4-fluorophenyl)-, N-benzyl-5-(4-nitrophenyl)-, and 5-phenyl-N-(4-tolyl)-1,3,4-thiadiazole-2-amines demonstrated higher inhibitory activities than cisplatin used as reference drug. The SAR analysis in this group showed that an aromatic ring and electronwithdrawing substituents promote anticancer activity [56]. Chandra et al (2019) synthesized and screened a series of novel 5-phenyl-substituted 1,3,4thiadiazole-2-amines for their antitumor and antitubercular activities.…”

Section: -83mentioning

confidence: 99%

Cytotoxic Properties of 1,3,4-Thiadiazole Derivatives—A Review

2020

View full text Add to dashboard Cite

show abstract

Section: -83mentioning

confidence: 99%

Cytotoxic Properties of 1,3,4-Thiadiazole Derivatives—A Review

2020

View full text Add to dashboard Cite

show abstract

“…The 1,3,4-thiadiazole was the isomer on which we concentrated due to their properties. The various biological activities of 1,3,4-thiadiazole are antimicrobial, , antituberculosis, anti-inflammatory, , carbonic anhydrase inhibitory, anticonvulsant, , antihypertensive, , antioxidant, , anticancer, , and antifungal properties. Drug molecules that contain 1,3,4-thiadiazole groups in their structures and their examples are given, e.g., carbonic anhydrase inhibitors acetazolamide and methazolamide .…”

Section: Introductionmentioning

confidence: 99%

New 1,3,4-Thiadiazole Derivatives as α-Glucosidase Inhibitors: Design, Synthesis, DFT, ADME, and In Vitro Enzymatic Studies

Ali,

Rehman,

Rasheed

et al. 2024

ACS Omega

View full text Add to dashboard Cite

Diabetes is an emerging disorder in the world and is caused due to the imbalance of insulin production as well as serious effects on the body. In search of a better treatment for diabetes, we designed a novel class of 1,3,4-thiadiazole-bearing Schiff base analogues and assessed them for the α-glucosidase enzyme. In the series (1−12), compounds are synthesized and 3 analogues showed excellent inhibitory activity against αglucosidase enzymes in the range of IC 50 values of 18.10 ± 0.20 to 1.10 ± 0.10 μM. In this series, analogues 4, 8, and 9 show remarkable inhibition profile IC 50 2.20 ± 0.10, 1.10 ± 0.10, and 1.30 ± 0.10 μM by using acarbose as a standard, whose IC 50 is 11.50 ± 0.30 μM. The structure of the synthesized compounds was confirmed through various spectroscopic techniques, such as NMR and HREI-MS. Additionally, molecular docking, pharmacokinetics, cytotoxic evaluation, and density functional theory study were performed to investigate their behavior.

show abstract

“…Some of the tested compounds showed promising antitumor activity in in vitro biological tests, exceeding the reference drugs in the tests. Many studies have also demonstrated the activity of compounds from this group against breast cancer cell lines [ 9 , 10 , 11 , 12 , 13 , 14 , 15 , 16 , 17 , 18 , 19 , 20 , 21 , 22 , 23 , 24 , 25 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Anticancer Activity of 1,3,4-Thiadiazoles with 3-Methoxyphenyl Substituent

et al. 2022

View full text Add to dashboard Cite

Based on the results of previous work, we designed and synthesized 1,3,4-thiadiazole derivatives. The cytotoxic activity of the obtained compounds was then determined in biological studies using MCF-7 and MDA-MB-231 breast cancer cells and a normal cell line (fibroblasts). The results showed that all compounds displayed weak anticancer activity towards two breast cancer lines: an estrogen-dependent cell line (MCF-7) and an estrogen-independent cell line (MDA-MB-231). The compound most active towards MCF-7 breast cancer cells was SCT-4, which decreased DNA biosynthesis to 70% ± 3 at 100 µM. The mechanism of the anticancer action of 1,3,4-thiadiazole was also investigated. We choose a set of the most investigated proteins, which are attractive anticancer targets. In silico studies demonstrated a possible multitarget mode of action for the synthesized compounds but the most likely mechanism of action for the new compounds is connected with the activity of caspase 8.

show abstract

Design and Synthesis of 1,3,4-Thiadiazole Derivatives as Novel Anticancer and Antitubercular Agents

Cited by 15 publications

References 25 publications

Cytotoxic Properties of 1,3,4-Thiadiazole Derivatives—A Review

Cytotoxic Properties of 1,3,4-Thiadiazole Derivatives—A Review

New 1,3,4-Thiadiazole Derivatives as α-Glucosidase Inhibitors: Design, Synthesis, DFT, ADME, and In Vitro Enzymatic Studies

Synthesis and Anticancer Activity of 1,3,4-Thiadiazoles with 3-Methoxyphenyl Substituent

Contact Info

Product

Resources

About