DNA binding studies of novel diazatruxenones analogs as potential anticancer agents: Synthesis, antitumor investigation, DNA binding, SAR and molecular modeling calculation

Synergistic effects of nanosized supramolecular complex inlaid with silver nanoparticles: Catalysis, sensors, and biological activities

“…DNA binding activity determination is very important as DNA is a vital target during the study of anticancer activities of the newly manufactured compounds. [ 84 ] Hereinafter, DNA methyl green displacement assay was carried out to investigate DNA binding activity of Ag/SC 1 nanocomposite. Methyl green reversibly binds polymerized DNA.…”

From truxenes to heterotruxenes: playing with heteroatoms and the symmetry of molecules

“…325 Consequently, the condensation of 56 was performed (Scheme 46). Subsequent studies also allowed condensation of 6-bromo 326 and 5-nitroindoles, 327 directly leading to doubly substituted 5,10-diazatruxenes. Moreover, the N-substituted indoles also undergo this reaction, allowing the direct synthesis of N-protected 5,10-diazatruxene-15-ones 140c , 324 and condensation using a stoichiometric amount of MeSO 3 H acid in 1,2-dichloroethane.…”

“…In the presence of a base, 140a and b undergo ionization, allowing reaction with various electrophiles, such as acyl chlorides, 325 simple alkyl halides, and more complex derivatives containing a piperidine or oxirane ring. 327 Alternatively, reducing the carbonyl group in 140c by treatment with N 2 H 4 in boiling ethylene glycol makes it possible to obtain the parent 5,10-diazatruxene 142 , 324 which after alkylation, is transformed to the highly soluble 143 (Scheme 47). Moreover, the presence of the carbonyl group enables the reaction between 140c and organometallic substances, leading to the appropriate 3° alcohols 141 (Scheme 46), significantly extending the functionalization possibilities of the 5,10-diazatruxene core.…”

The synthesis of indole-3-carbinols (I3C) and their application to access unsymmetrical bis(3-indolyl)methanes (BIMs) bearing a quaternary sp3-carbon

“…4,5 In particular, indole-3-carbinol, a bioactive key chemical component in all vegetables of the Cruciferae family, is an important motif, as it possess a high potency to bind with DNA and, therefore, has anti-carcinogenic activity. 6 Moreover, these molecules are promising synthetic precursors for the construction of various simple to complex biologically important heterocyclic building blocks. 7…”

“…On the other hand, bis(3-indolyl)methanes (BIMs), another class of bioactive molecules, are generated metabolically by the condensation of I3C (the major product of the hydrolysis of indole-GLSs) in the acidic pH of the stomach. 6,10 a These molecules exhibit strong inhibitory effects on phenobarbital induced hepatic cyp-mRNA expression 10 b and anti-cancer activity. 10 c Despite several methods being developed for the synthesis of symmetrical bis(indolyl)methanes, 11 the preparation of unsymmetrical bis(indolyl)methanes containing an sp 3 carbon are still limited.…”