Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Abstract

This review article proposes a comprehensive report of the design strategies engaged in the development of various sulfur-bearing cytotoxic agents. The outcomes of various studies depict that the sulfur heterocyclic framework is a fundamental structure in diverse synthetic analogs representing a myriad scope of therapeutic activities. A number of five-, six-and seven-membered sulfur-containing heterocyclic scaffolds, such as thiazoles, thiadiazoles, thiazolidinediones, thiophenes, thiopyrans, benzothiazoles, benzothiophenes, thienopyrimidines, simple and modified phenothiazines, and thiazepines have been discussed. The subsequent studies of the derivatives unveiled their cytotoxic effects through multiple mechanisms (viz. inhibition of tyrosine kinases, topoisomerase I and II, tubulin, COX, DNA synthesis, and PI3K/Akt and Raf/MEK/ERK signaling pathways), and several others. Thus, our concise illustration explains the design strategy and anticancer potential of these five-and six-membered sulfur-containing heterocyclic molecules along with a brief outline on seven-membered sulfur heterocycles. The thorough assessment of antiproliferative activities with the reference drug allows a proficient assessment of the structure-activity relationships (SARs) of the diversely synthesized molecules of the series.

Research Progress in Synthesis and Application of Thiosulfonates

“…22). 机理研 究表明, 该反应可能是铜卡宾先与硫代磺酸酯反应得到 硫叶立德中间体, 其再发生 [1,2] 光照条件下, 芳基重氮化合物可作为自由基前体与 硫代磺酸酯发生取代反应, 生成芳基硫醚, 其中芳基是 前者提供的, 烷硫基来自于硫代磺酸酯 [98] . 通常, 芳基 重氮四氟硼酸盐是芳基自由基前体(Eq.…”

“…In the future, among the researches on the construction of new sulfides with thiosulfonates, various difunctionalization reactions are still promising directions. Keywords thiosulfonate; green chemistry; C-S bond formation; photocatalysis; radical reaction; difunctionalization reaction 含硫有机化合物广泛出现在天然产物 [1] 、合成药 物 [2] 、 荧光探针 [3] 等分子中, 在诸多领域都有着十分广泛 的应用 [4] . 硫代磺酸酯是一种特殊的硫化物, 它包含一 个氧化态为 II 的硫原子和另一个氧化态为 VI 的硫原子, 这使它们能够与亲核试剂和亲电试剂反应 [5] .…”

Contribution of Knoevenagel Condensation Products toward the Development of Anticancer Agents: An Updated Review

“…Chemotherapy is one of the practical approaches in annihilating tumour growth and eradicating cancer. The development of novel anticancer drugs with a different mode of action, impressive potency, favourable pharmacokinetics, good safety profiles and reduced side effects is needed to complement the current chemotherapeutic strategies [1–13] …”

Thioarylation of anilines using dual catalysis: two-step synthesis of phenothiazines

“…Phenothiazine heterocycles are an important structural motif, found as the core component of a wide range of pharmaceutically active agents. 1,2 Early analogues such as the parent compound, phenothiazine (Fig. 1) was used as an anthelmintic agent in livestock and humans, 3 while the dye, methylene blue was used for the treatment of malaria.…”