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Molecules 2018, 23, 1436 2 of 13 Molecules 2018, 23, x FOR PEER REVIEW 2 of 13 into the market [4,5]. Up to now, most current work focuses on the improvement of porphyrin and chlorin-type PS molecules and, especially, synthesis of new type of PSs with high water solubility, into the market [4,5]. Up to now, most current work focuses on the improvement of porphyrin and strong absorption in near-infrared region, and long half-life [2,6]. chlorin-type PS molecules and, especially, synthesis of new type of PSs with high water solubility, During our continuing project for developing new generation of PSs [7–10], the strong absorption in near-infrared region, and long half-life [2,6]. benzo[a]pDhuerniongxazoiunriumconcthinlouriindgespdryojesctcamforetodeovuelroaptitnegntinoenwdugeentoertahtieoinrgofodPpShsot[o7s–t1a0b],ilithy,ehigh benzo[a]phenoxazinium chlorides dyes came to our attention due to their good photostability, high molar absorption, long-wavelength absorption, and relative low fluorescence quantum yield [11–13]. molar absorption, long-wavelength absorption, and relative low fluorescence quantum yield [11–13]. Literature survey indicated that benzo[a]phenoxazinium derivatives exhibited antifungal [12,14], Literature survey indicated that benzo[a]phenoxazinium derivatives exhibited antifungal [12,14], and and antimalarial activity [15], and especially functioned as PSs in antimicrobial PDT [15–18]. However, antimalarial activity [15], and especially functioned as PSs in antimicrobial PDT [15–18]. However, to to our knowledge, the potential anticancer PDT of benzo[a]phenoxazinium dyes has been little our knowledge, the potential anticancer PDT of benzo[a]phenoxazinium dyes has been little investigated [19]. In this context, the main objective of the present work was to design and synthesize investigated [19]. In this context, the main objective of the present work was to design and synthesize several new benzo[a]phenoxazinium chlorides PS1–PS5 (Figure 1) and investigate their potential several new benzo[a]phenoxazinium chlorides PS1–PS5 (Figure 1) and investigate their potential anticancer photodynamic activity. anticancer photodynamic activity. Figure 1. Structures of benzo[a]phenoxazinium chlorides PS1–PS5. Figure 1. Structures of benzo[a]phenoxazinium chlorides PS1–PS5. 2. Results and Discussion 2. Results and Discussion 2.1. Design and Synthesis 2.1. Design and Synthesis The ligand-mediated targeting (LMT) strategy in PDT has been explored to increase the efficacy Tahndelriegdauncde-amdevderiaseteedffteacrtsgeotfinPgSs(L[2M].TIn)sthtreatpergesyenintsPtDudTyh,faisvebebenzeox[pa]lpohrendotxoazininciruemascehtlhoreideeffiscacy andrpeodsuscesesiandgvdeirffserenftfefuctnsctoiofnPaSlsfra[2g]m.eIntsthatethpere5s-aemntinsotupdosyi,tifionvewbereendzeos[iag]npehdeanodxparzeipnaiuremdbcahsleodrides on the LMT strategy. PS1 was a simple known benzo[a]phenoxazinium derivative with methyl possessing different functional fragments at the 5-amino position were designed and prepared based propionate reported by Frade et al. [13,14,20], which was shown to have antimicrobial activity against on the LMT strategy. PS1 was a simple known benzo[a]phenoxazinium derivative with methyl Saccharomyces cerevisiae [14], but its anticancer PDT had not yet been investigated. Other compounds propionate reported by Frade et al. [13,14,20], which was shown to have antimicrobial activity against are new synthetic benzo[a]phenoxazinium derivatives: PS2 possesses a morpholinoethylamine Saccharomyces cerevisiae [14], but its anticancer PDT had not yet been investigated. Other compounds moiety, which is a well-known ligand for targeting lysosome [21]; PS3 is equipped with a biotin are new synthetic benzo[a]phenoxazinium derivatives: PS2 possesses a morpholinoethylamine moiety, moiety, which is a well-known tumor-targeting molecule [22] and has been used for selective delivery which is a well-known ligand for targeting lysosome [21]; PS3 is equipped with a biotin moiety, which of PS to cancer tissues [23,24]; PS4 was a conjugate of benzo[a]phenoxazinium and pregnenolone. is a well-known tumor-targeting molecule [22] and has been used for selective delivery of PS to cancer Pregnenolone, known as a precursor to most hormones, had been explored as carrier of anticancer tissuedsru[2g3s,2[245]];. PInSa4dwdiatisona, cseovnejruaglatytepeosfobfepnrezgon[ae]npohloeneodxearzivinatiiuvmes wanedreprerpegorntednotolohnaev.ePanretigcnanecneorlone, knowanctiavsityabpyreocuurrasnodrotothemrogsrotuhposr[m26o–n2e8]s.,PhSa5dwbaesesnynethxepsliozreeddasasthceafrirsiterbeonfzoa[nat]pichaencoexrazdinruiugms[25]. dimer to determine the superimposed effect of the benzo[a]phenoxazinium core on anticancer PDT In addition, several types of pregnenolone derivatives were reported to have anticancer activity by our The synthetic routes for target compounds PS1 to PS5 are depicted in Schemes 1–5, respectively. the superimposed effect of the benzo[a]phenoxazinium core on anticancer PDT efficacy. Briefly, compound 2 was synthesized by alkylation of 1-naphthylamine (1) with 3-bromopropanoic The synthetic routes for target compounds PS1 to PS5 are depicted in Schemes 1–5, respectively. Briefly, compound 2 was synthesized by alkylation of 1-naphthylamine (1) with 3-bromopropanoic acid, efficacy. and other groups [26–28]. PS5 was synthesized as the first benzo[a]phenoxazinium dimer to determinePDF Image | Photosensitizers for Anticancer Photodynamic Therapy
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