Gul'nara V. Giniyatullina's research while affiliated with Russian Academy of Sciences and other places

... Further, as 1,4-diazepane is hydrophobic, facilitate the organotin complex to permeate the cell and enhance the compound's biological activity [7]. In medicinal chemistry, 1,4-diazepane moiety has shown extensive pharmaceutical properties ( Fig. 1) as anti-HIV [8,9], anti-dengue [10], anti-Alzheimer [11], anti-tubercular [12], anti-fungal [13], anti-oxidant [14,15], anti-bacterial [16], anti-cancer [17], anti-microbial [13,18], Histamine receptor [19], anti-tumour [7,20], and as Kinase inhibitor [21]. Further, piperidine is a fundamental heterocyclic part of medical chemistry. ...

... Betulin, betulinic acid, and betulonic acid are pentacyclic triterpenoids found in over 200 plant species [19,20]. Betulinic acid, betulonic acid, and their derivatives possess a wide range of pharmacological effects, including anti-HIV, anti-parasitic, anti-inflammatory, and anti-tumor effects [20][21][22][23][24][25][26]. Since betulinic acid is poorly soluble in aqueous solutions, it is frequently derivatized to promote solubility and improve the pharmacological activity [27][28][29]. ...

... The metabolism and total clearance are important parameters when evaluating drug pharmacokinetic [105]. As shown in the results, all the lead compounds from PEHc revealed good pharmacokinetic-related values that are useful in drug design. ...

... At the same time triterpenes holding a modified Aring are less studied; for example, 3-propyloxy-ursolic acid showed K i = 4.29 μM (Loesche, Köwitsch, et al., 2019) and glycyrrhetol and betulin A-ring azepanes gave K i values 0.21 and 0.35 μM, respectively (Kazakova et al., 2020). ...

... Previously [6], we studied the kinetics of the antioxidant action of new triterpenoids of the lupane series and identified their mechanism of action, including the reaction of regeneration of the original antioxidant. At the same time, it is known that triterpenoids and derivatives based on them exhibit antiviral and antitumor activity [7][8][9][10]. Among the native triterpenoids of the lupane series, betulinic acid has the highest activity [11], in connection with which, in this work, the antioxidant properties of betulinic acid derivatives AO1-AO4 have been studied (Fig. 1). ...

... Our previous studies confirm that compounds containing such groups as isonicotinic, methoxycinnamic, succinic, polyamine, arylidene, amide, propargylaminoalkyl, and azepane display cytotoxic and antimicrobial activity [25,26]. Also, we have shown that among the different types of triterpenoids [27][28][29], 2,3-indolo-betulinic acid glycine and L-phenylalanine amides were discovered as lead compounds with IC 50 values of 0.04 and 0.05 µM, being 3784-and 4730-fold more active than acarbose [30]. Triterpene type indoles were highlighted as excellent pharmacophore platforms for the development of new anti-diabetes drugs [31]. ...

... Thus, acetylenyl derivatives of the natural pentacyclic triterpenoid betulin demonstrated antitumor activity in a large panel of human cancer cell lines which was 2-3 times better than betulinic acid [10,11]. Moreover, betulin derivatives with the carbon-carbon triple bond at the C19 atom significantly inhibited herpes virus (HSV) replication, although no antiviral activity was observed in betulin itself [12]. The addition of the carbon-carbon triple bond to the heterocyclic moiety or the sugar residue of nucleoside analogues provided them with powerful antiproliferative action caused by dose-dependent DNA damage [13,14] and antiviral activity against RNA viruses [15]. ...