8‐Hydroxyquinoline, being one of the privileged scaffolds, is known to possess a wide range of biological activities. 8‐Hydroxyquinoline quinoline has been explored synthetically through functionalization at different positions by different groups in search of medicinally important molecules. Herein, we synthesized twenty‐one (20 a‐20 u) different hydrazones of 8‐hydroxyquinoline at C‐2 position in good yields and characterised by 1H NMR, 13C NMR, HRMS and IR. All the synthesized compounds were evaluated for their anti‐HIV‐1 and anti‐cancer potential through in vitro cell‐based assays. Compound 20 u ((E)‐2‐((2‐(4‐methoxyphenyl)hydrazono)methyl)quinolin‐8‐ol) was found to be the most active against HIV (IC50: 1.88 and 6.27 μM; TI 73.82 and 22.07, against HIV‐1VB59 and HIV‐1UG070 respectively). Compound 20 l ((E)‐2‐((2‐(4‐fluorophenyl)hydrazono)methyl)quinolin‐8‐ol) was identified as the most cytotoxic against four cancer cell lines (IC50: 26.30, 34.19, 38.77 and 34.23 μM against HeLa, MCF‐7, A‐549 and MDA‐MB‐231, respectively) with 2.4, 1.9, 1.6, 1.9‐folds selectivity, respectively over normal cells (IC50 63.75 μM against HEK‐293 normal cells).

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Highly active anti-retroviral therapy (HAART) is prescribed for HIV infection and, to a certain extent, limits the infection’s spread. However, it cannot completely eradicate the latent virus in remote and cellular reservoir areas, and due to the complex nature of the infection, the total eradication of HIV is difficult to achieve. Furthermore, monotherapy and multiple therapies are not of much help. Hence, there is a dire need for novel drug delivery strategies that may improve efficacy, decrease side effects, reduce dosing frequency, and improve patient adherence to therapy. Such a novel strategy could help to target the reservoir sites and eradicate HIV from different biological sanctuaries. In the current review, we have described HIV pathogenesis, the mechanism of HIV replication, and different biological reservoir sites to better understand the underlying mechanisms of HIV spread. Further, the review deliberates on the challenges faced by the current conventional drug delivery systems and introduces some novel drug delivery strategies that have been explored to overcome conventional drug delivery limitations. In addition, the review also summarizes several nanotechnology-based approaches that are being explored to resolve the challenges of HIV treatment by the virtue of delivering a variety of anti-HIV agents, either as combination therapies or by actively targeting HIV reservoir sites.