Synthesis and antitumor activity of daunorubicin conjugates with of 3,4-methylendioxybenzaldehyde

Biomimetic Magnetite Nanoparticles as Targeted Drug Nanocarriers and Mediators of Hyperthermia in an Experimental Cancer Model

“…It can enter the mitochondria, causing DNA damage and energetic stress, by activating the caspase cascade, leading to cell death by apoptosis and triggering autophagy as a consequence of cell energy depletion. Finally, it can translocate into the nucleus, where it intercalates between double-stranded DNA helices and inhibits the enzymes topoisomerases I and II, provoking lethal changes in chromatin structure and the generation of free radicals which, when combined with iron ions, induce oxidative damage to cellular membranes, DNA, and proteins [6][7][8][9]. However, DOXO treatments can induce severe cardiotoxicity due to DOXO accumulation in cardiac tissue [10], which then imposes a narrow therapeutic dose, thus limiting DOXO effectiveness [11].…”

Design and synthesis of hybrid compounds as novel drugs and medicines

“…The analogues linked with an amide spacer were shown to be 100-times less toxic to normal healthy cells and had lower anticancer activity compared to analogues linked with an amine spacer, which showed higher toxicity both to healthy and to the four cancer cell lines. 24 …”

“…With their wide variety of cellular effects, polyamine containing hybrid compounds may yet be useful agents in the chemoprevention of cancer. 23 Brel and co-workerrs 24 showed that covalently linking cancerostatic daunorubicin and a natural antiproliferative agent, piperonal and its dimethoxy derivative by a simple amine spacer makes a designed conjugate with higher anticancer activity compared to an amide spacer synthesised from piperonylic acid (Fig. 4).…”

“…The analogues linked with an amide spacer were shown to be 100-times less toxic to normal healthy cells and had lower anticancer activity compared to analogues linked with an amine spacer, which showed higher toxicity both to healthy and to the four cancer cell lines. 24 Benzylcoumarin has good anticancer activity by inhibiting several targets, e.g., 17b-HSD3, MEK1, and NQO1. [25][26][27] Wang et al reported the synthesis of a series of coumarinbenzimidazole analogues.…”

The Role of Intestinal Flora in Anti-Tumor Antibiotic Therapy

“…Chimeric molecules were formed by connecting two different pharmacophores with spacers [126], which helped in eliminating the toxic effects of anthracycline antibiotics. With advances in chemical and biosynthetic engineering, some natural active substances, such as patamycin, which have significant biological activities, but are not applied as therapeutic agents due to their strong cytotoxicity, have potential for clinical applications [127]. Toxicity reduction and efficacy enhancement in antibiotic treatment of tumors can be achieved through molecular structural modification [64,122,126,127] and drug combination therapy [123][124][125].…”