Novel diosgenin derivatives containing 1,3,4-oxadiazole/thiadiazole moieties as potential antitumor agents: Design, synthesis and cytotoxic evaluation

Synthesis and In Vitro Antitumor Evaluation of Some Carbazole‐Based Thiazole, Thiophene, and 1,3,4‐Thiadiazole Derivatives

“…The downfield appearance of hydrazone-NH proton may be ascribed to the involving of NH proton in intramolecular hydrogen bond with C=O group. The 13 C-NMR spectrum revealed three sp 3 In a similar manner, treatment of 20 with chloroacetonitrile (23) in boiling ethanolic triethylamine solution yielded 4-((9ethyl-9H-carbazol-3-yl)diazenyl)-3-methyl-5-(phenylamino) thiophene-2-carbonitrile (24). The structure of the latter product was established on the basis of microanalysis and spectral data.…”

“…[16] On the other hand, the antiproliferative carbazole derivative EHop-016 acts as Rac1 inhibitor. [17] Besides carbazoles, thiophene, [18][19][20] 1,3-thiazole [21][22][23] and 1,3,4-thiadiazole [24][25][26] derivatives are acquiring a lot of interest as central cores in drug design and in particular as promising templates for the development of new and more efficient anticancer agents that can solve or at least minimize major problems such as drug resistance, toxicity, or other adverse side effects.…”

Novel Steroidal 5α,8α-Endoperoxide Derivatives with Semicarbazone/Thiosemicarbazone Side-chain as Apoptotic Inducers through an Intrinsic Apoptosis Pathway: Design, Synthesis and Biological Studies

“…The interesting structural and stereochemical features of the steroid nucleus provide system and side chains [13]. The interesting structural and stereochemical features of the steroid nucleus provide additional fascination for researchers, and the introduction of heteroatoms, heterocycles, or amides, or replacement of one or more carbon atoms in the steroidal skeleton has been envisaged to discover new chemical entities with the potential to become promising future drugs, resulting in notable modifications in biological activity [14][15][16]. Ergosterol peroxide (5α,8α-epidioxiergosta-6,22-dien-3β-ol, EP) is a member of a class of fungal secondary metaboliters of sterol 5α,8α-endoperoxidederivatives ( Figure 2).…”

Synthesis and antitumor activity of new isolated and fused heterobicyclic nitrogen systems containing 1,3,4-thiadiazole moiety derived from N1,N2-diaryl hydrazine compound

“…Recently, functionally 1,2,4-triazine derivatives showed an important biological activity such as anti-HIV, and anticancer [21], antioxidant [22], anti-inflammatory [23], antifungal [24], herbicidal [25] and antibacterial [26,27] agents. Also, 1,3,4thiadiazoles containingsmall heterocyclic nitrogen nucleus exhibited a greatspectrum biological activity as anti-inflammatory [28], anticancer [29,30], antimicrobial [31,32], anti-HIV, and antitumor [33], and antimycotic [34] agents. Based on these important observations, the present research gives a combination of small heterocyclic nitrogen molecules with 1,3,4-thiadiazole moiety to getnovel isolated and/ or fused heteropolycyclic systems as thiazolo-1,2,4-triazines in view of their antitumor activity.…”