A series of substituted quinolines was screened for their antiproliferative, cytotoxic, antibacterial activities, DNA/protein binding affinity, and anticholinergic properties by using the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide cell proliferation, lactate dehydrogenase cytotoxicity, and microdilution assays, the Wolfe–Shimmer equality method, the Ellman method, and the esterase assay, respectively. The results of the cytotoxic and anticancer activities of the compounds displayed that 6‐bromotetrahydroquinoline (2), 6,8‐dibromotetrahydroquinoline (3), 8‐bromo‐6‐cyanoquinoline (10), 5‐bromo‐6,8‐dimethoxyquinoline (12), the novel N‐nitrated 6,8‐dimethoxyquinoline (13), and 5,7‐dibromo‐8‐hydroxyquinoline (17) showed a significant antiproliferative potency against the A549, HeLa, HT29, Hep3B, and MCF7 cancer cell lines (IC50 = 2–50 μg/ml) and low cytotoxicity (∼7–35%) as the controls, 5‐fluorouracil and cisplatin. The compound–DNA linkages are hyperchromic or hypochromic, causing variations in their spectra. This situation shows that they can be bound to DNA with the groove‐binding mode, with Kb value in the range of 2.0 × 103–2.2 × 105 M–1. Studies on human Gram(+) and Gram(−) pathogenic bacteria showed that the substituted quinolines exhibited selective antimicrobial activities with MIC values of 62.50–250 μg/ml. All tested quinoline derivatives were found to be effective inhibitors of acetylcholinesterase (AChE) and the human carbonic anhydrase I and II isoforms (hCA I and II), with Ki values of 46.04–956.82 nM for hCA I, 54.95–976.93 nM for hCA II, and 5.51–155.22 nM for AChE. As a result, the preliminary data showed that substituted quinolines displayed effective pharmacological features. Molecular docking studies were performed to investigate the binding modes and interaction energies for compounds 2–17 with AChE (PDB ID: 4EY6), hCA I (PDB ID: 1BMZ), and hCA II (PDB ID: 2ABE).

Two novel cyanido-complexes having very significant antibacterial, antifungal and anticancer activities in vitro were synthesized and characterized using various techniques.

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The synthesis, characterization and biological activity of three novel dicyanidoargentate(i)-based complexes are reported. The in vitro results show that these complexes may be potent antiproliferative drug candidates.

Four new dicyanoargentate(I)-based complexes 1-4 were synthesized from certain metal ions with a tetradentate ligand [N, N-bis (2-hydroxyethyl)-ethylenediamine; N-bishydeten] and determined by diverse procedures (elemental, thermal, FT-IR, ESI-MS for 1-3 and, magnetic susceptibility and EPR for 1, and 2) including crystal analysis of 4. The crystal method revealed that complex 4 has a sandwich-type like polymeric chemical structure with layers formed by [Cd(N-bishydeten) 2 ] 2+ cations and [Ag(CN) 2 ] − anions. The complexes were further characterized by fluorescence and UV spectroscopy to determine their physicochemical features. The complexes displayed a DNA binding activity within the same range as found for cisplatin, in addition to their strong stability in the presence of the physiological buffer system. The complexes were also investigated for pharmacological properties like interaction with DNA/Bovine serum albumin, anticancer and antibacterial activities. Physicochemical studies of DNA with the complexes suggested that the interaction mode between them are possibly both intercalative and groove binding types. These spectroscopic measurements also show that there may be a binding tendency between BSA and the complexes via hydrogen or Van der Waals bonds. The viability tests demonstrated that all the complexes exhibited antibacterial (1-4) and anticancer effects (2-4) toward ten diverse bacterial strains and three tumor cells (HT-29 colon adenocarcinoma, HeLa cervical cancer, and C6 glioma), respectively. Despite the current advances in cancer therapy, the death rate from cancer and therapeutic agents are still increasing 1. A significant number of studies have focused on the synthesis and design of a new antiproliferative agent to reduce the risk of drug resistance and cell toxicity 2-4. Some of these studies are related to metallo compounds which constitute a significant part of agents with potent pharmacological activities, and their medicinal availability has been still explored 5,6. For example, some macrocyclic polyamines containing Ni, Cu, and Ru could recognize TAR RNA molecules and cleave them, and affect the interaction of Tat-RNA 7. Mn(II) complex of 2H-5-hydroxy-1,2,5-oxadiazo[3,4-f]1,10-phenanthroline has significant antitumor activity against HL-60, KB, Hela and BGC-823 cells.

The protic molten salts (PMOS) of (1 a-6 b) have been prepared from the reactions of tetrapyrrolidino (1-3) and tetrapiperidino (4-6) fully substituted phosphazenes with the gentisic and gresorcylic acids. The structures of PMOS (1 a-6 b) were characterized by elemental analyses, FTIR and 1 H, 13 C{ 1 H}, 31 P{ 1 H} NMR techniques. The crystal structures of 1 b and 2 b were established by X-ray diffraction method. The thermal properties of PMOS were verified using thermogravimetric instruments. In addition, this study also focused on the pharmacological abilities of the PMOS to affect the cell growth and cell cytotoxicity on A549, Hep3B and normal human amnion (FL) cell lines and to interact with calf thymus DNA (CT-DNA).Studies on the cells displayed that these PMOS demonstrated significant antiproliferative effect in conjunction with caused apoptotic-like changes in morphology. The PMOS are able to strongly bind to CT-DNA through minor groove binding modes with hyperchromic effect. The IC 50 and binding constant ranges of the PMOS were found to be as 25-160 mM and 0.5 x 10 3 À12.0 x 10 3 M À1 , respectively. These findings indicate that the PMOS 1 b-6 b are more antiproliferative than those of the PMOS 1 a-6 a. Moreover, it is observed that the CT-DNA most significantly bound the PMOS 1 b-6 b. Consequently, a good correlation between the antiproliferative effects and their binding activities of these PMOS was observed.

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