Synthesis of novel 16-spiro steroids: Spiro-7′-(aryl)tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazolo-trans-androsterone hybrid heterocycles

Synthesis, anti-inflammatory and anti-ulcer evaluations of thiazole, thiophene, pyridine and pyran derivatives derived from androstenedione

“…Although much attention has been directed to study the biological importance of androstenedione [23][24][25][26] no investigations have appeared in the literature to describe its uses in heterocyclic synthesis. Therefore, the need to create novel androstenedione derivatives for emerging drug targets is an active area of medicinal chemistry.…”

Anti-inflammatory and Anti-ulcer Activities of New Fused Thiazole Derivatives Derived from 2-(2-Oxo-2H-chromen-3-yl)thiazol-4(5H)-one

“…22 Results are given in Table 4 for the compounds which exhibited optimal anti-inflammatory and anti-ulcer activity, that is the eleven compounds 7b, 8a, 10a, 10b, 13a, 13b, 15b, 18a, 19b, 19c and 19d. The shrimp lethality assay is considered as a useful tool for preliminary assessment of toxicity, and it has been used for the detection of fungal toxins, plant extract toxicity, heavy metals, cyanobacteria toxins, pesticides, and cytotoxicity testing of dental materials, 23 natural and synthetic organic compounds. 24 It has also been shown that A. salina toxicity test results have a correlation with rodent and human acute oral toxicity data.…”

The Knoevenagel reactions of pregnenolone with cyanomethylene reagents: Synthesis of thiophene, thieno[2,3-b]pyridine, thieno[3,2-d]isoxazole derivatives of pregnenolone and their in vitro cytotoxicity towards tumor and normal cell lines

“…Thus, a solution of compound 6 (E/Z) reacted with hydrazine hydrate (7) to give the pyrazole derivative 8. In addition, its reaction with phenyl hydrazine (9) gave the pyrazole derivative 10. Compounds 8 and 10 exist also in the E/Z forms which were separated using column chromatography to give 8a (E), 8b (Z) and 10a (E) and 10b (Z), respectively (see experimental section).…”

“…Chemical modification of the steroid D-ring provides a way to alter the functional groups, sizes and stereochemistry of the D-ring, and numerous structure-activity relationships have been established by such synthetic alterations. Steroids bearing heterocycles fused to the D-ring of the steroid nucleus have been of pharmaceutical interest [9][10][11]. The syntheses of abirateron [17-(3-pyridyl)androst-5,16-dien-3-ol] and its 4-en-3-one analog were reported recently; these display high inhibitory activities against 17a-hydroxylase/C17,20-lyase (P45017).…”