1,3,4-Thiadiazoles of pharmacological interest: Recent trends in their synthesis via tandem 1,3-dipolar cycloaddition: Review

Thiazoles and 1,3,4-thiadiazoles have been reported to possess various pharmacological activities. A novel series of thiazoles carrying 1,3,4-thiadiazole core were designed and prepared via the reaction of the 2-(4-methyl-2-phenylthiazole-5-carbonyl)-N-phenylhydrazinecarbo-thioamide with the appropriate hydrazonoyl chlorides. The structures of the newly synthesized compounds were confirmed based on elemental and spectral analysis as well as their alternative syntheses. The cytotoxic potency of the newly synthesized thiadiazoles was evaluated by their growth inhibitory potency in liver HepG2 cancer cell line. Also, the structure activity relationship was studied. All the newly synthesized compounds were evaluated for their anticancer activity against liver carcinoma cell line (HepG2) using MTT assay. The results revealed that the compounds 12d, 12c, 6g, 18b, 6c, and 6f (IC50 = 0.82, 0.91, 1.06, 1.25, 1.29 and 1.88 µM, respectively) had good antitumor activity against liver carcinoma cell line (HepG2) when compared with the standard drug Doxorubicin (IC50 = 0.72 µM).

/pdf/a-facile-synthesis-and-anticancer-activity-of-some-novel-4dl6izc45t.pdf

A facile synthesis and anticancer activity of some novel thiazoles carrying 1,3,4-thiadiazole moiety.

SZC015, a synthetic oleanolic acid derivative, induces both apoptosis and autophagy in MCF-7 breast cancer cells.

Methyl 3-hydroxyimino-11-oxoolean-12-en-28-oate (HIMOXOL), a synthetic oleanolic acid derivative, induces both apoptosis and autophagy in MDA-MB-231 breast cancer cells

Background Nowadays, cancer is an important public health problem in all countries. Limitations of current chemotherapy for neoplastic diseases such as severe adverse reactions and tumor resistance to the chemotherapeutic drugs have been led to a temptation for focusing on the discovery and development of new compounds with potential anticancer activity. The importance of thiophene and thiadiazole rings as scaffolds present in a wide range of therapeutic agents has been well reported and has driven the synthesis of a large number of novel antitumor agents. Methods A series of new 1,3,4-thiadiazoles were synthesized by heterocyclization of N-(4-nitrophenyl)thiophene-2-carbohydrazonoyl chloride with a variety of hydrazine-carbodithioate derivatives. The mechanisms of these reactions were discussed and the structure of the new products was elucidated via spectral data and elemental analysis. All the new synthesized compounds were investigated for in vitro activities against human hepatocellular carcinoma (HepG-2) and human lung cancer (A-549) cell lines compared with cisplatin standard anticancer drug. Moreover, molecular docking using MOE 2014.09 software was also carried out for the high potent compound 20b with the binding site of dihydrofolate reductase (DHFR, PDB ID (3NU0)). Results The results showed that compound 20b has promising activities against HepG-2 and A-549 cell lines (IC50 value of 4.37±0.7 and 8.03±0.5 μM, respectively) and the results of molecular docking supported the biological activity with total binding energy equals -1.6 E (Kcal/mol). Conclusion Overall, we synthesized a new series of 1,3,4-thiadiazoles as potential antitumor agents against HepG-2 and A-549 cell lines.

/pdf/5-thiophen-2-yl-1-3-4-thiadiazole-derivatives-synthesis-3fqt86z9ko.pdf

5-(Thiophen-2-yl)-1,3,4-thiadiazole derivatives: synthesis, molecular docking and in vitro cytotoxicity evaluation as potential anticancer agents.

Article history: Received on: 21/05/2015 Revised on: 13/09/2015 Accepted on: 02/11/2015 Available online: 10/03/2016 Among bicyclic non-aromatic nitrogen heterocycles, phthalimides are an interesting class of compounds with a large range of applications. Phthalimide contains an imide functional group and may be considered as nitrogen analogues of anhydrides or as diacyl derivatives of ammonia. They are lipophilic and neutral compounds and can therefore easily cross biological membranes in vivo and showing different pharmacological activities. In the present work compounds containing phthalimide subunit have been described as a scaffold to design new prototypes drug candidates with different biological activities and are used in different diseases as, for example AIDS, tumor, diabetes, multiple myeloma, convulsion, inflammation, pain, bacterial infection among others.

/pdf/recent-advances-and-future-prospects-of-phthalimide-1wb99gyzl9.pdf

Recent Advances and Future Prospects of Phthalimide Derivatives

Thiadiazole and its derivatives are important organic reaction intermediates and they have been widely used as anticonvulsan t, antidepressan t, analgesic, antiinflammatory, antiplatelet, antimalarial, antimicrobial, antimycobacterial, antitumoral, antiviral, diuretic and muscles relaxant activity. Generally, synthesis of the thiadiazole derivations needs high temperature (≥ 100 0 C) or low t emp erature (< 0 0 C) or high pressure (at least

/pdf/biological-activities-of-thiadiazole-derivatives-a-review-2ypxoii0ju.pdf

Biological Activities of Thiadiazole Derivatives: A Review

The efficacy and safety of any pharmaceutical product is determined by the compounds (desired and undesired) which it contains The purpose of quality control is to ensure that each dosage unit of the drug product delivers the same amount of active ingredients and is, as far as possible, free of impurities As herbal medicinal products are complex mixtures which originate from biological sources, great efforts are necessary to guarantee a constant and adequate quality By carefully selecting the plant material and a standardized manufacturing process the pattern and concentration of constituents of herbal medicinal products should be kept as constant as possible as this is a prerequisite for reproducible therapeutic results

/pdf/role-of-markers-in-the-standardization-of-herbal-drugs-a-1brvmas9as.pdf

Role of markers in the standardization of herbal drugs: a review.

Triazine is the six-membered heterocyclic ring containing three nitrogens, which replace the carbon-hydrogen unit in the benzene ring. Based on nitrogen position present in the ring system, it is categorized in three isomeric forms, i.e., 1, 2, 3-triazine (vicinal triazine), 1, 2, 4-triazine (asymmetrical triazine or isotriazine) and 1, 3, 5-triazine (symmetrical or s-triazine or cyanidine). Triazines have a weakly basic property. Their isomers have much weaker resonance energy than benzene structure, so nucleophilic substitution reactions are more preferred than electrophilic substitution reactions. Triazine isomers and their derivatives are known to play important roles possessing various activities in medicinal and agricultural fields such as anti-cancer, antiviral, fungicidal, insecticidal, bactericidal, herbicidal, antimalarial and antimicrobial agents.

The Chemistry of Triazine Isomers: Structures, Reactions, Synthesis and Applications.

Recently, naturally occurring and abundantly available halloysite nanoclay has emerged as a nanomaterial carrier system suitable for both controlled and sustained delivery. These aluminosilicate tubes of 50-nm diameter, with outer silica and inner alumina layers, possess a tubular structure, with excellent features such as large aspect ratio, good biocompatibility, and high mechanical strength entails them to be suitable for drug delivery. The unique features of these nanotubes are the ability to load DNA and enzyme due to opposite charges on both inner and outer surfaces which allow selective drug loading on both surfaces. This review article emphasizes on the drug loading techniques with release characteristics and some important applications in biomedical, environmental fields, and different types of medication. Being most versatile, these nanotubes can be used widely as a carrier system for enzyme bases and different types of the nucleus which can be a most promising step for novel drug delivery systems.

Neelottama Kushwaha

Papers

Recent Advances and Future Prospects of Phthalimide Derivatives

Biological Activities of Thiadiazole Derivatives: A Review

Role of markers in the standardization of herbal drugs: a review.

The Chemistry of Triazine Isomers: Structures, Reactions, Synthesis and Applications.

Halloysite Nanotubes for Nanomedicine: Prospects, Challenges and Applications