Synthesis and antituberculosis activity of some new pyridazine derivatives. Part II

Synthesis, structure, antimycobacterial and anticancer evaluation of new pyrrolo-phenanthroline derivatives

“…In the same time, benzo[c]phenanthridinium alkaloids as fagaronine and nitidine which showed antileukemic activity on rodents 44 and act as topoisomerase I and II inhibitors [45][46][47] , played the role of model compound for the development of new anticancer agents 14 . Having all these above consideration in mind and encouraged by our previous promising results in the field of anti-TB [25][26][27][28] and anticancer 29,30,32 derivatives with indolizine and/or phenanthroline skeleton, we have focused on the design of novel structures that contain four or five fused (hetero)cycles with pyrrolo[2,1-c] [4,7]phenanthroline skeleton (Scheme 3). In equal measure, we were interested to see the influence of the substituents at pyrrolo ring (especially the pharmacophoric moiety p-chloro-benzoyl 26 ) on the pharmacological properties, and if the increasing of number of fused rings from four to five will affect these properties (Scheme 3).…”

“…As part of our ongoing research in the field of design and synthesis of new anti-TB [25][26][27][28] and anticancer derivatives [29][30][31][32] with azaheterocycles skeleton, we report here the design, synthesis, structure and in vitro antimycobacterial and anticancer evaluation of new class of compounds with pyrrolo [2,1-c] [4,7]phenanthroline scaffold. To the best of our knowledge, there is no previous report, concerning the synthesis of pyrrolo [2,1-c] [4,7]-phenanthroline derivatives.…”

Antitubercular Drugs Development: Recent Advances in Selected Therapeutic Targets and Rational Drug Design

“…In these compounds a relationship between Br, Cl and CH 3 substituents, respectively, with Br and vinyl has been found with a favorable anti-TB activity. In these compounds there is an influence of the substituents X in para-position on the aromatic ring, where the activity is increased in the following order: CH 3 < Cl < Br with the activity being affected by the R1 substituents, where the most active compounds have a CH 3 group (55, figure 18) (Mantu et al, 2010). …”

Hybrid imidazole (benzimidazole)/pyridine (quinoline) derivatives and evaluation of their anticancer and antimycobacterial activity

“…In previously research work, we successfully identify azaheterocycles derivatives (imidazole/benzimidazole and pyridine/quinoline included) with anticancer 9,10,[16][17][18][19] and anti-TB [15][16][17][20][21][22][23] activity. In the light of the above consideration, it appears rational to combine the pharmacophoric potential of the two core scaffolds, imidazole (and its benzo-derivative benzimidazole) and pyridine (and its benzo-derivative quinoline), intending to obtain new entities with better anticancer and antimycobacterial activity and, also, with better pharmaceutical properties (i.e.…”

“…; anticancer [5][6][7][8][9][10] and anti-TB 11-15 also included). Encouraged by the above considerations and in continuation of our research in the area of novel anticancer 9,10,[16][17][18][19] and anti-TB [15][16][17][20][21][22][23] derivatives with azaheterocyclic skeleton, we report here the design, synthesis, structure, and in vitro anticancer and antimycobacterial activity of new hybrid imidazole (benzimidazole)/pyridine (quinoline) derivatives.…”