Abstract
The 1,3,4-thiadiazole derivatives (9a–i) were synthesized under solvent free conditions and their chemical composition was confirmed using different spectral tools (IR, Mass, and NMR spectrometry). All the synthesized compounds were screened for their anti-cancer potentiality over human breast carcinoma (MCF-7) and human lung carcinoma (A-549). Most of the tested compounds showed remarkable anti-breast cancer activity. However, compound 4 showed the most anti-lung cancer activity. Then, compounds with cytotoxic activity ≥ 80% over breast and lung cells were subjected to investigate their specificity on human normal skin cell line (BJ-1). Compounds 9b and 9g were chosen owing to their high breast anti-cancer efficacy and their safety, in order to study the possible anti-cancer mode of action. Otherwise, drug delivery provides a means to overcome the low solubility, un-targeted release, and limited bioavailability of the prepared 1,3,4-thiadiazole drug-like substances. Compounds 9b and 9g were chosen to be encapsulated in Na-alginate microspheres. The release profile and mechanism of both compounds were investigated, and the results revealed that the release profiles of both microspheres showed a sustained release, and the release mechanism was controlled by Fickian diffusion. Accordingly, these compounds are promising for their use in chemotherapy for cancer treatment, and their hydrophilicity was improved by polymer encapsulation to become more effective in their pharmaceutical application.
Highlights
Cancer is one of the major causes of death today [1]
The release profile and mechanism of both compounds were investigated, and the results revealed that the release profiles of both microspheres showed a sustained release, and the release mechanism was controlled by Fickian diffusion
The chemical composition of 4 was confirmed via chemical transformation. It was reacted with a series of selected derivatives of hydrazonoyl halides by grinding in the presence of 2–3 drops of DIPEA (N,N-Diisopropylethylamine) to give products assigned as 1-5-(3-(1(4-bromophenyl)-5-methyl-1H-1,2,3-triazol-4-yl)-1-phenyl-1H-pyrazol-4yl)methylene)hydrazono)-4-4,5-dihydro-1,3,4-thiadiazol-2-yl) derivatives (9a–i) (Scheme 1) based on their spectral and micro-analytical data
Summary
Cancer is one of the major causes of death today [1]. There are three main ways for treatment of cancer—Either individually or combined; surgery, chemotherapy, and radiation. Chemotherapy is a common method for cancer treatment [2]. Investigation of novel structures, designing and synthesis of some new, potent, and less toxic anti-cancer agents remains a major challenge for medical chemists. The 1,3,4-Thiadiazoles- and 1,2,3-Triazole-based heterocycles have been well exploited for the production of many new medicinal scaffolds. The 1,3,4-Thiadiazole ring system is one of the Molecules 2019, 24, 2371; doi:10.3390/molecules24132371 www.mdpi.com/journal/molecules
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